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|
 | increases intracellular Ca2++ concentrations 12791703(C)
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| BH3-mimetic compound ABT737 (Oltersdorf et al, 2005)
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|
 | Transcription inhibitor that binds DNA at the transcription initiation complex and preventing elongation by RNA polymerase [Wiki].
|
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| Sobell H (1985). "Actinomycin and DNA transcription". Proc Natl Acad Sci U S A 82 (16): 5328-31. PMID 2410919.
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| a chemotherapeutic drug which at low doses elicits a strong p53 response. 9727636(C)
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| Ac-Trp-Glu-His-Asp-7-Amino-4-Methylcoumarin
|
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| (Cat.# AMC156)
A fluorogenic substrate for detecting caspase-1, caspase-4, and caspase-5 activity.
Excitation max.: 365–380 nm, Emission max.: 430–460 nm
Thornberry, N.A. et al., J. Biol. Chem., 272:17907 (1997)
Thornberry, N.A., and Lazebnik, Y. 1998. Science 281, 1312.
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| a caspase-1 inhibitor 15507117(C)
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| 17360653(C): Casp1 inhibitor
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| theoretical substrate for AMP formation resulting in AMPK activation 14978242(C)
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| DNA-damaging agent 12654725(C)
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| aka Doxorubicin hydroxyldaunorubicin
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| anthracycline antibiotic [Wiki]
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| a bridged compound based on the caspase-9 amino terminus, which was linked via the thre-
onine at the P2-position 18570872(C)
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| Aegera Therapeutics Inc., 810 Chemin du Golf, Ile de Soeurs, Quebec H3E1A8, Canada
|
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| decreases protein expression of Ciap1 Ciap2 and Xiap within 20 min 18570872-Fig-3b
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| a pore forming toxin from Aeromonas hydrophila 17186029(C)
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| induces potassium efflux and activateds caspase-1 inflammasome in a Nalp3-dependent manners 16990137(D)
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| EGFR kinase inhibitor 15950906(C) 16806820(C)
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| a specific inhibitor of EGFR kinase 14657239
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| EGFR kinase IC50=3 nM [Calbio]
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| ErbB2 kinase IC50>100um [Calbio]
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| PDGFRkinase IC50>100 uM [Calbio]
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| Jak2/Stat kinase inhibitor 15950906(C)
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| selective tyrosine kinase inhibitors for ErbB2 19393267(C)
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| SID 26758181 Calbiochem #124005
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| 1L6-Hydroxymethyl-chiro-inositol-2-(R)-2-O-methyl-3-O-octadecyl-sn-glycerocarbonate
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| A phosphatidylinositol ether analog that potently and selectively inhibits Akt (PKB) (IC50 of 5.0 µM). Moderately inhibits PI 3-K activity (IC50 = 83.0 µM). Also inhibits the growth of various cancer cell lines with IC50 values in the 1 - 10 µM range
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| Ref.: Hu, Y., et al. 2000 J. Med. Chem. 43, 3045.
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| Calbiochem 208721 Calpain inhibitor II
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| Cell permeable inhibitor of calpain I (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 600 pM). Inhibits activation-induced programmed cell death and restores defective immune responses in HIV+ donors. Blocks nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene. A weak inhibitor of proteasome.
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| Protease inhibitor 11518704(C)
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| N-acetyl-leucine-leucine-methionine
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| Allnal
Calpain inhibitor I
LLNL
N-Ac-Leu-leu-norleucinal
CID4332, IN1502, IN1511
Ac-LLnL-CHO
MG-101, MG 101, MG101
N-Acetyl-Leu-Leu-Norleu-al
N-Acetyl-L-leucyl-L-leucyl-L-norleucinal
Acetyl-leucinyl-leucinyl-norleucinal (CI-I)
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| inhibitor of adenosine kinase (Adk) 16497986(C)
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| 5'-amino-5'-deoxyadenosine p-toluensulfonate
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| inhibitor of macropinocytosis 12393678(C)
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| Alcohol ester derivatives of amino acids freely diffuse across membranes and, within the cytoplasm and lysosomes, are hydrolyzed by esterases into native amino acids (15). 22053050(C)
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| 15. J. P. Reeves, J. Biol. Chem. 254, 8914 (1979).
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| phosphodiesterase III inhibitor resulting in accumulation of cyclic AMP [6283063] 14978242(C)
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| acetyltransferase inhibitor 17074756(C)
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| 11069105(C) inhibitor of oxidative phosphorylation
|
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| 12150925(C) an electron transport inhibitor
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| Wolvetang, E.J., Johnson, K.L., Krauer, K., Ralph, S.J., and Linnane,
A.W. (1994). Mitochondrial respiratory chain inhibitors induce apoptosis. FEBS Lett. 339, 40–44.
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| Mitochondrial metabolic inhibitor 17277771(C)
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| adenosine-5'alpha,beta-methylene diphosphate
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| To exclude the possible adenosine effect in nucleotide-induced AMPK activation, we inhibited 5'-nucleotidase 16497986(C)
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|
| FKBP12 binds to the naturally occurring product FK506 and can be homodimerized with FK1012, which consists of two linked molecules of FK506 (31). A synthetic, cell-permeable homodimerizing reagent, AP20187, which has a greatly reduced affinity for endogenous FKBP12 (~250 nM), binds with high affinity (~0.1 nM) to a F36V mutant (Fv) form of FKBP12 (32).
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| 31. Spencer, D. M., Wandless, T. J., Schreiber, S. L., and Crabtree, G. R. (1993) Science 262, 1019 –1024
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| 32. Clackson, T., Yang, W., Rozamus, L. W., Hatada, M., Amara, J. F., Rollins, C. T., Stevenson, L. F., Magari, S. R., Wood, S. A., Courage, N. L., Lu, X., Cerasoli, F., Jr., Gilman, M., and Holt, D. A. (1998) Proc. Natl. Acad. Sci. U. S. A. 95, 10437–10442
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|
| Aphidicolin is defined as a tetracyclic diterpene antibiotic with antiviral and antimitotical properties. Aphidicolin is a reversible inhibitor of eukaryotic nuclear DNA replication. It blocks the cell cycle at early S phase. It is a specific inhibitor of DNA polymerase A,D in eukaryotic cells and in some viruses and an apoptosis inducer in HeLa cells. Natural aphidicolin is a secondary metabolite of the fungus Nigrospora oryzae. [Wikipedia]
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| sodium-meta-arsenite NaAsO2
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| JNK/SAPK activator arsenite (45) 10232608(C)
|
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| 38. Chen, C., and Okayama, H. High-efficiency transformation of mammalian cells by
plasmid DNA. Mol. Cell. Biol., 7: 2745–2752, 1987.
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| Arsenic chloride 19276070(C)
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| accumulates autophagosomes under starvation conditions 11060023(C)
|
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| Inhibits fusion between autophogosomes and lysosomes 11060023(C)->Hoyvik 1986
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| inhibitor of acidification of the endosomes 12900525(C)
|
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| neutralizes endosomal pH 15711573(C)
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| inhibitor of intracellular Ca2+ 16497986(C)
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| 1,2-bis-(o-aminophenoxy)ethane-N,N,N,N-tetraacetic acid tetraacetoxy-methyl ester
|
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|
| a chemical inhibitor of Ikba phosphorylation (49)
|
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| 49. Pierce, J. W., Schoenleber, R., Jesmok, G., Best, J., Moore, S. A., Collins, T., and Gerritsen, M. E. (1997) J. Biol. Chem. 272, 21096–21103
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| IKK inhibitor 15485931(C)
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| 27. Pierce, J. W., R. Schoenleber, G. Jesmock, J. Best, S. A. Moore, T. Collins, and M. E. Gerritsen. 1997. Novel inhibitors of cytokine-induced I��B�� phos- phorylation and endothelial cell adhesion molecule expression show anti- inflammatory effect in vivo. J. Biol. Chem. 272:21096–21103.
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|
| A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase [Pubchem]
|
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| beta-(+/-)-2-aminobicyclo-(2,2,1)-heptane-2-carboxylic acid
|
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| non-metabolizable analog of leucine
|
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|
| an inhibitor of SLC7A5 (Kanai et al., 1998; Mastroberardino et al., 1998; Yanagida et al., 2001) 19203585(C)
|
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| Kanai, Y., Segawa, H., Miyamoto, K., Uchino, H., Takeda, E., and Endou, H. (1998). Expression cloning and characterization of a transporter for large neutral amino acids activated by the heavy chain of 4F2 antigen (CD98). J. Biol. Chem. 273, 23629–23632.
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| Yanagida, O., Kanai, Y., Chairoungdua, A., Kim, D.K., Segawa, H., Nii, T., Cha, S.H., Matsuo, H., Fukushima, J., Fukasawa, Y., et al. (2001). Human L-type
amino acid transporter 1 (LAT1): characterization of function and expression in tumor cell lines. Biochim. Biophys. Acta 1514, 291–302.
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|
|
|
| [t-butoxy carbonyl-Asp-fluoromethylketone; abbr. also: BAF, BD-fmk, BD, Boc-D] This compound is a general inhibitor of caspases. It is cell-permeable and inhibits cell death by apoptosis induced by a variety of stimuli in various cell types by preventing the activation of proforms of caspases into their bioactive form (Cheng et al, 1998; Deshmukh et al, 1996; McCarthy et al, 1997). LAST MODIFIED: January 2004
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|
| REFERENCES: Cheng Y et al Caspase inhibitor affords neuroprotection with delayed administration in a rat model of neonatal hypoxic-ischemic brain injury. Journal of Clinical Investigation 101(9): 1992-1999 (1998); Deshmukh M et al Genetic and metabolic status of NGF-deprived sympathetic neurons saved by an inhibitor of ICE family proteases. Journal of Cell Biology 135(5): 1341-1354 (1996); McCarthy NJ et al Inhibition of Ced-3/ICE-related proteases does not prevent cell death induced by oncogenes, DNA damage, or the Bcl-2 homologue Bak. Journal of Cell Biology 136(1): 215-227 (1997)
|
|
|
|
| a caspase inhibitor from Enzyme Systems (aka MPbio) 10753878(C)
|
|
|
|
| possibly Boc-Asp(OMe)-Fluoromethylketone
|
|
|
|
| synonyms: Boc-Asp(OMe)-FMK Boc-D9Ome)-FMK
|
|
|
|
| Rsk inhibitor 19274086(C)
|
|
|
|
| Calbiiochem 203290 Bisindolylmaleimide I
|
|
|
|
| 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, GF 109203X, Gö 6850
|
|
|
|
| A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC50 = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα-, βI-, βII-, γ-, δ-, and ε- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK-3β immunoprecipitates (IC50 = 170 nM). May inhibit protein kinase A at a much higher concentration (IC50 = 2 µM).
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|
| Protein kinase C inhibitor 15485654(C)
|
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|
|
| Inhibits PKCa PKCb1 PKCb2 PKCg PKCd PKCe 11278339-D
|
|
|
|
| pan-P38 inhibitor 18458086
|
|
|
|
| 32. Kuma, Y., Sabio, G., Bain, J., Shpiro, N., Marquez, R., and Cuenda, A.
(2005) J. Biol. Chem. 280, 19472–19479
|
|
|
|
| Bleomycin is a glycopeptide antibiotic produced by the bacterium Streptomyces verticillus. Bleomycin refers to a family of structurally related compounds. When used as an anticancer agent, the chemotherapeutical forms are primarily bleomycin A2 and B2. It works by causing breaks in DNA.
Wikipedia
|
|
|
|
| stimulates TLR1/TLR2 15241416(C)
|
|
|
|
| 401480 IKK Inhibitor III, BMS-345541 Calbiochem
|
|
|
|
| 4-(2′-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
|
|
|
|
| A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
|
|
|
|
| a 14-amino-acid peptide: Pyr-Gln-Arg-Leu-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2
|
|
|
|
| NFkb inhibitor; a modified dipeptidyl boronic acid from Ortho Biotech, Neuss, Germany 16533170(C)
|
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|
|
| PS-341, Velcade, MG-341, ProScript
|
|
|
|
| Wiki: proteasome inhibitor
|
|
|
|
| inhibits Arf GDP-GTP exchange 9520417(C)
|
|
|
|
| disrupts Golgi apparatus 16880211(C)
|
|
|
|
| Brefeldin A reversibly inhibits the small GTPase Arf, which leads to retraction of the Golgi membranes back into the ER (17, 27). 12324469(C)
|
|
|
|
| 17. Lippincott-Schwartz, J. (2001) Histochem. Cell Biol. 116, 97–107
27. Ward, T. (2001) J. Cell Biol. 155, 557–570
|
|
|
|
| BFA has been shown to affect intracellular trafficking dramatically by disintegrating the Golgi apparatus and endosomes (Tooze and Hollinshead, 1992; Wood and Brown, 1992; Faundez et al., 1997), cellular compartments that contain Rap1 (Kim et al., 1990; Beranger et al., 1991). 11466412(C)
|
|
|
|
| Beranger F, Goud B, Tavitian A, de Gunzburg J (1991) Association of the Ras-antagoni stic Rap1/ Krev-1 proteins with the Golgi complex. Proc Natl Acad Sci USA 88:1606–1610.
Faundez V, Horng J-T, Kelly RB (1997) ADP ribosylation factor 1 is required for synaptic vesicle budding in PC12 cells. J Cell Biol 138:505–515.
Kim S, Mizoguchi A, Kikuchi A, Takai Y (1990) Tissue and subcellular distributions of the smg-21/ Rap1/ Krev-1 proteins which are partly distinct from those of c-Ras p21s. Mol Cell Biol 10:2645–2652.
Tooze J, Hollinshead M (1992) In AtT20 and HeLa cells brefeldin A induces the fusion of tubular endosomes and changes their distribution and some of their endocytic properties. J Cell Biol 118:813– 830.
Wood SA, Brown WJ (1992) The morphology but not the function of endosomes and lysosomes is altered by brefeldin A. J Cell Biol 119:273–285.
|
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|
|
| Thiazolidenedione ligand for PPARg
|
|
|
|
| transcriptional activation of acyl-CoA oxidase promoter construct
|
|
|
|
| Pparg agonist 11009565(C)
|
|
|
|
| an IAP antagonist 18621737(C)
|
|
|
|
| 23. Varfolomeev, E., Blankenship, J. W., Wayson, S. M., Fedorova, A. V., Kayagaki, N., Garg, P., Zobel, K., Dynek, J. N., Elliott, L. O., Wallweber, H. J., Flygare, J. A., Fairbrother, W. J., Deshayes, K., Dixit, V. M., and Vucic, D. (2007) Cell 131, 669 – 681
|
|
|
|
| agonist for P2X and P2Y11 receptors 16497986(C)
|
|
|
|
| 2',3'-O-(4-benzoylbenzoyl)-ATP
|
|
|
|
| 26 N-hexanoylsphingosine 9020886(C)
|
|
|
|
| induces a slow increased in Ca2+ , autophagy, and autophagy-dependent cell death 17244528(C)
|
|
|
|
| tha active form of vitamin D3
|
|
|
|
| an analog of 1,25-dihydroxyvitamin D3 which induces a slow increased in Ca2+ , autophagy, and autophagy-dependent cell death 17244528(C)
|
|
|
|
| "1,25-(OH)2vitamin D3" an agonist for VdR 16143103(D)
|
|
|
|
| Calmodulin antagonist 11397791(C)
|
|
|
|
| Calphostin C, Cladosporium cladosporioides, UCN-1028c
|
|
|
|
| A cell permeable, highly specific inhibitor of protein kinase C (IC50 = 50 nM) that interacts with the protein’s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. Does not compete with Ca2+ or phospholipids. At higher concentrations inhibits myosin light chain kinase (IC50 > 5 µM), protein kinase A (IC50 > 50 µM), protein kinase G (IC50 > 25 µM), and p60v-src (IC50 > 50 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Requires brief exposure to light for activation. Purity: ≥95% by HPLC. CAS 121263-19-2.
Ref.: Jarvis, W.D., et al. 1994. Cancer Res. 54, 1707. Svetlov, S., and Nigami, S. 1993. Biochim. Biophys. Acta 1177, 75. Gopalakrishna, R., et al. 1992. FEBS Lett. 314, 149. Shimamato, H., et al. 1992. Br. J. Pharmacol. 107, 282. Bruns, R.F., et al. 1991. Biochem. Biophys. Res. Commun. 176, 288. Tamaoki, T., et al. 1990. Biotechnology 8, 732. Kobayashi, E., et al. 1989. Biochem. Biophys. Res. Commun. 159, 548.
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|
| PucChem CIDs: 5311365 5280780 5890287 5459084 356334
|
|
|
|
| Calyculin A is reported to inhibit PP1 more selectively than PP2A [10692405] 11292821(C)
|
|
|
|
| causes cofilin dephos in neutrophils 12451591(DA)
|
|
|
|
| Inhibits PP2A cataylic subunit - not acid or alkaline phosphatases, or PTPases [2539153]
|
|
|
|
| 7629157(D) induces phos of Ikba
|
|
|
|
| 15485932(D) Ser/Thr phosphatases induces insulin resistance
|
|
|
|
| inhibits both PP1 and PP2a families 17079228(C)
|
|
|
|
| a phosphatase inhibitor for protein phosphatase (PP) 1 and PP2A (50)
|
|
|
|
| 50. Sun, S. C., Maggirwar, S. B., and Harhaj, E. (1995) J. Biol. Chem. 270,
18347–18351
|
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|
|
| Calbiochem 208851 Calyculin A, Discodermia calyx
|
|
|
|
| A cell-permeable inhibitor of protein phosphatase 2A (PP2A; IC50 = 0.5-1 nM) and protein phosphatase 1 (PP1; IC50 = 2 nM). A non-phorbol ester type tumor promoter that induces oxidative DNA damage. Selectively increases the efficacy of AMPA receptor-mediated synaptic transmission at excitatory synapses. Also known to prevent γ-radiation induced apoptosis in Burkitt’s lymphoma cell line BM13674.
|
|
|
|
| DNA-damaging agent 16571722(C)
|
|
|
|
| DNA topoisomerase inhibitor (CalBio)
|
|
|
|
| Induces apopotosis 16260609
|
|
|
|
| Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). [Wikipedia]
|
|
|
|
| A slowly hydrolyzed cholinergic agonist that acts at both muscarinic and nicotinic receptors
|
|
|
|
| An anticonvulsant used to control grand mal and psychomotor or focal seizures. Its mode of action is not fully understood, but some of its actions resemble those of PHENYTOIN; although there is little chemical resemblance between the two compounds, their three-dimensional structure is similar.
|
|
|
|
| 17446862(C) autophagy inducer
|
|
|
|
| Carbonyl cyanide 3-chlorophenylhydrazone
|
|
|
|
| Inhibits ATP production via irreversible dissipation of the electrochemical gradient 17459875(C)
|
|
|
|
| Cadmium chloride 19276070(C)
|
|
|
|
| MLK inhibitor 16687404(C)
|
|
|
|
| specificity: 15923109(D) 15878863(D) 15525794(D)
|
|
|
|
| MLK inhibitor 16230351(C)
|
|
|
|
| 30. Maroney, A. C., Finn, J. P., Connors, T. J., Durkin, J. T., Angeles, T., Gessner, G., Xu, Z., Meyer, S. L., Savage, M. J., Greene, L. A., Scott, R. W., and Vaught, J. L. (2001) J. Biol. Chem. 276, 25302–25308
|
|
|
|
| whereas ceramide associates preferably with the trans-Golgi
complex (43)
|
|
|
|
| 3-N-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine
|
|
|
|
| inhibits the mitogen-activated protein kinase-interacting kinase Mnk1 [Pubchem]
|
|
|
|
| Src inhibitor 17646016(C)
|
|
|
|
| AdoRa2a selective agonist 12082090(C)
|
|
|
|
| chelerythrine chloride, a nonspecific PKC inhibitor 10330161(C)
|
|
|
|
| inhibits formation of clathrin-coated pits 15247273(C)
|
|
|
|
| Wang, LH (1993) J. Cell Biol. 123, 1107–1117
|
|
|
|
| inhibits protein degradation by lysosomes 11163210(C)
|
|
|
|
| Chloroquine inhibits maturation of early endosomes to lysosomes by inhibiting acidification and thus preventing lysosomal degradation (Mellman et al, 1986).
|
|
|
|
| Mellman I, Fuchs R, Helenius A (1986) Acidiication of the endocytic and exocytic pathways. Annu Rev Biochem 55: 663–700
|
|
|
|
| inhibitor of acidification of the endosomes 12900525(C)
|
|
|
|
| The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup
|
|
|
|
| chloro-radicicol A (chlrad A) Tak1 inhibitor 22069318(C)
|
|
|
|
| Broad profiling of this pharmacophore against a panel of 401 kinases showed it to be a potent and irreversible inhibitor of the following kinases: TAK1, VEGFR, FLT3, GAK, KIT, MEK, MKNK, PDGFR, PRKD, STK36, TGFR (18).
|
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|
|
| 17. Dakas, P. Y., Barluenga, S., Totzke, F., Zirrgiebel, U., and Winssinger, N. (2007) Angew
Chem Int Ed Engl 46, 6899-6902
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| 18. Jogireddy, R., Dakas, P. Y., Valot, G., Barluenga, S., and Winssinger, N. (2009) Chemistry
15, 11498-11506
|
|
|
|
| Cycloheximide is an inhibitor of protein biosynthesis in eukaryotic organisms, produced by the bacterium Streptomyces griseus. Cycloheximide exerts its effect by interfering with the translocation step in protein synthesis (movement of two tRNA molecules and mRNA in relation to the ribosome) thus blocking translational elongation.
|
|
|
|
| Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis
|
|
|
|
| Mek inhibitor 19187764(C)
|
|
|
|
| aka CI-1040, CI 1040, PD-184352, PD184352, PD 184352, 2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide
|
|
|
|
| casein kinase I inhibitor
|
|
|
|
| N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide
|
|
|
|
| CNI-1493, a tetravalent guanylhydrazone compound, has been shown to inhibit the production of proinflammatory cytokines by monocytic/macrophage cells in response to lipopolysaccharide (46). The inhibition of proinflammatory cytokineproduction appears to operate at a post-transcriptional level(47), and there is some preliminary evidence to suggest that CNI-1493 is able to inhibit activation of p38 MAP kinase (48).
|
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|
|
| 46. Bianchi, M., Bloom, O., Raabe, T., Cohen, P. S., Chesney, J., Sherry, B., Schmidtmayerova, H., Calandra, T., Zhang, X., Bukrinsky, M., Ulrich, P., Cerami, A., and Tracey, K. J. (1996) J. Exp. Med. 183, 927–936
|
|
|
|
| 47. Cohen, P. S., Nakshatri, H., Dennis, J., Caragine, T., Bianchi, M., Cerami, A., and Tracey, K. J. (1996) Proc. Natl. Acad. Sci. U. S. A. 93, 3967–3971
|
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|
| 48. Cohen, P. S., Schmidtmayerova, H., Dennis, J., Dubrovsky, L., Sherry, B., Wang, H., Bukrinsky, M., and Tracey, K. J. (1997) Mol. Med. 3, 339–346
|
|
|
|
| Tpl2 inhibitor 19754427(C)
|
|
|
|
| 19 Miyoshi, J., Higashi, T., Mukai, H., Ohuchi, T. and Kakunaga, T. (1991) Structure and
transforming potential of the human cot oncogene encoding a putative protein kinase.
Mol. Cell. Biol. 11, 4088–4096
|
|
|
|
| synthetic E.coli typ Lipid-A 10435584(C)
|
|
|
|
| EGFR specific inhibitor 17646016(C)
|
|
|
|
| compound 56
PD153035 Analog 56
CID2857
IN1496
K00042
4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline
|
|
|
|
| ConA is known to label the rough endoplasmic reticulum and the dilated cisternae of the cis-Golgi apparatus structure
|
|
|
|
| Winqvist, L (1979) J. Cell Sci. 39, 101–116
|
|
|
|
| Antibiotic which is a specific inhibitor of vacuolar H+ ATPase. More potent & specific inhibitor than Bafilomycin A1. Inhibits the acidification of organelles including lysosomes and the Golgi apparatus. Reported to block cell surface expression of viral glycoproteins without affecting synthesis. Exhibits cytotoxic effects in a number of cell lines in a cell viability assay. Structurally related to Bafilomycins, B1183 & B1185.
|
|
|
|
| inhibitor of the v-ATPase that does not have other known targets (11–14). 22053050(C)
|
|
|
|
| 11. M. Forgac, Nat. Rev. Mol. Cell Biol. 8, 917 (2007).
|
|
|
|
| 12. B. J. Bowman, M. E. McCall, R. Baertsch, E. J. Bowman,
J. Biol. Chem. 281, 31885 (2006).
|
|
|
|
| 13. M. R. Boyd et al., J. Pharmacol. Exp. Ther. 297, 114
(2001).
|
|
|
|
| 14. M. Huss et al., J. Biol. Chem. 277, 40544 (2002).
|
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|
|
| used to dimerize proteins tagged with bacterial gyrase B (GyrB)
|
|
|
|
| Src family kinase inhibitor
|
|
|
|
| 10. Hanke, J. H., J. P. Gardner, R. L. Dow, P. S. Changelian, W. H. Brissette,E. J. Weringer, B. A. Pollok, and P. A. Connelly. 1996. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J. Biol. Chem. 271:695–701.
|
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|
| synthetic oligodeoxynucleotides of approx 8−30 bases in length that contain one or more CpG motifs of unmethylated CpG dinucleotides in certain base contexts
|
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|
|
| used as a ligand for TLR9
|
|
|
|
| Sequences are from 5' to 3';
lowercase letters represent phosphorothioate linkage;
uppercase letters represent phosphodiester linkage 3' of the base;
bold letters represent CpG dinucleotides.
|
|
|
|
| used in: 11812998 11130078
|
|
|
|
| tcctggcggggaagt (inhibitory)
|
|
|
|
| ACCGATAACGTTGCCGGTGACGGCACCACG
|
|
|
|
| 23. Gursel, I., M. Gursel, H. Yamada, K. J. Ishii, F. Takeshita, and D. M. Klinman. 2003. Repetitive elements in mammalian telomeres suppress bacterial DNA-induced immune activation. J. Immunol. 171:1393.
|
|
|
|
| used in: 15800576 16306936
|
|
|
|
| uppercase letters indicate phosphorothioates and lowercase letters indicate phosphodiesters
|
|
|
|
| 9. Verthelyi, D., K. J. Ishii, M. Gursel, F. Takeshita, and D. M. Klinman. 2001. Human peripheral blood cells differentially recognize and respond to two distinct CpG motifs. J. Immunol. 166:2372.
|
|
|
|
| negative control: gGTGCATCTATGCAGGGGgg
|
|
|
|
| uppercase letters indicate phosphorothioates and lowercase letters indicate phosphodiesters
|
|
|
|
| 22. Yamada, H., I. Gursel, F. Takeshita, J. Conover, K. J. Ishii, M. Gursel, S. Takeshita, and D. M. Klinman. 2002. Effect of suppressive DNA on CpG- induced immune activation. J. Immunol. 169:5590.
|
|
|
|
| ATCGACTCTCGAGCGTTCTC
flip control: ATGCACTCTGCAGGCTTCTC
|
|
|
|
| uppercase letters indicate phosphorothioates and lowercase letters indicate phosphodiesters
|
|
|
|
| 2. Takeshita, F., C. A. Leifer, I. Gursel, K. J. Ishii, S. Takeshita, M. Gursel, and D. M. Klinman. 2001. Cutting edge: role of Toll-like receptor 9 in CpG DNA-induced activation of human cells. J. Immunol. 167:3555.
|
|
|
|
| negative control: tcaagtgttctc
|
|
|
|
| Wiki: binds to ganglioside GM1
|
|
|
|
| used for visualizing GM1-gangliosides in lipid rafts 16880211(D)
|
|
|
|
| used in 14716310 without explanation
|
|
|
|
| generates constitutively active Gnas 16303557(C)
|
|
|
|
| kinase inhibitor 18456659(C)
|
|
|
|
| beta-cyclodextrin is known to disrupt cholesterol-rich caveolae 18356165(C)
|
|
|
|
| synonyms: Cyclosporin-A, CsA
|
|
|
|
| inhibits calcineurin 17519230(C)
|
|
|
|
| inhibits PP2B 17079228(C)
|
|
|
|
| Calbiochem 239835 Cyclosporin A, Tolypocladium inflatum
|
|
|
|
| Cyclic oligopeptide with immunosuppressant properties. Induces apoptosis in rat thymocytes and in the murine B cell lymphoma cell line, WEH1-231. However, prevents anti-IgM and ionomycin-induced apoptosis in BLB cell lines. The complex of cyclosporin A with cyclophilin inhibits protein phosphatase 2B with nanomolar affinity. Inhibits nitric oxide synthesis induced by interleukin-1α, lipopolysaccharides, and TNF-α. Induces cardiomyocytes from embryonic stem cells.
|
|
|
|
| Cytosine-beta-D-arabinofuranoside
|
|
|
|
| Shortens actin filaments by blocking monomer addition at the fast-growing end of polymers
|
|
|
|
| a specific agonist for OpRd1 16325578(C)
|
|
|
|
| partial agonist for OpRk1
|
|
|
|
| Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.
|
|
|
|
| ROS in cells cause oxidation of DCFH, yielding the fluorescent product
2,7-dichlorofluorescein (DCF) 15265871(C)
|
|
|
|
| 2',7'-dichlorofluorescein diacetate
|
|
|
|
| DEL-1 (CEISEAYRGDTFIGYVCK), a peptide that specifically induces the clustering of integrin avb3 even in cells in suspension (Penta et al., 1999) 16760434(C)
|
|
|
|
| Penta, K., Varner, J. A., Liaw, L., Hidai, C., Schatzman, R., and Quertermous, T. (1999). Del1 induces integrin signaling and angiogenesis by ligation of alphaVbeta3. J. Biol. Chem. 274, 11101–11109.
|
|
|
|
| a specific agonist for OpRd1 16325578(C)
|
|
|
|
| H-Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2
|
|
|
|
| A selective δ-opioid receptor agonist isolated from the skin of Phyllomedusa bicolor.
|
|
|
|
| a Casp3 inhibitor 10692572(C)
|
|
|
|
| glucocorticoid receptor (GR) agonist 16143103(C)
|
|
|
|
| marker for generation of ROS - oxidation products fluoresce
|
|
|
|
| a selective, competitive inhibitor of SphkS [1310683] 12626530(C)
|
|
|
|
| PubChem CIDs: 5353800,4278
|
|
|
|
| A sulfhydryl reagent which oxidizes sulfhydryl groups to the disulfide form. It is a radiation-sensitizing agent of anoxic bacterial and mammalian cells.
|
|
|
|
| 9564042(C): a sulfhydryl-specific oxidant
|
|
|
|
| binds to the KATP-channel maintaining it in an open conformation [12615955(R)] 17287212(C)
|
|
|
|
| blocks insulin release by inhibiting the influx of extracellular Ca2+ 17287212(C)
|
|
|
|
| A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
|
|
|
|
| N6,2'-O-dibutyryl adenosine 3',5'-cyclic monophosphate sodium 10455189(C)
|
|
|
|
| desferrioxamine B, desferoxamine B, DFO-B, DFOA, DFB or desferal
|
|
|
|
| Deferoxamine is a bacterial siderophore produced by the actinobacteria Streptomyces pilosus. It has medical applications as a chelating agent used to remove excess iron from the body.[1] The mesylate salt of DFO-B is commercially available. Wikipedia
|
|
|
|
| Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. Pubchem
|
|
|
|
| an inhibitor of JNK signaling 15142038(C)
|
|
|
|
| a phosphodiesterase V/VI inhibitor 17292863(C)
|
|
|
|
| contraction mimetic 17292863(C)
|
|
|
|
| aka 2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole, CK2 Inhibitor II
|
|
|
|
| CK2 inhibitor 18678890(C)
|
|
|
|
| 26. Pagano MA, et al. (2004) 2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole: A
novel powerful and selective inhibitor of protein kinase CK2. Biochem Biophys Res
Commun 321:1040–1044.
|
|
|
|
| 2,3-dimethoxy-1,4-naphthoquinone
|
|
|
|
| penetrates the plasma membrane and releases O2�� inside the cell (22).
|
|
|
|
| 22. Dypbukt, J. M., Ankarcrona, M., Burkitt, M., Sjoholm, A., Strom, K., Orrenius,
S., and Nicotera, P. (1994) J. Biol. Chem. 269, 30553–30560
|
|
|
|
| dimethyloxallyl glycine CID 560326
|
|
|
|
| PHD inhibitor 19762779(C)
|
|
|
|
| 1-chloro-2,4-dinitrobenzene
|
|
|
|
| 9564042(C): an electrophilic compound which acts as a specific inhibitor of Trx
reductase (Novogrodsky et al., 1979; Arner et al., 1995) and thus increases the oxidized form of Trx in vivo.
|
|
|
|
| Novogrodsky,A., Nehring,R.E.J. and Meister,A. (1979) Inhibition of
amino acid transport into lymphoid cells by the glutamine analog L-2-
amino-4-oxo-5-chloropentanoate. Proc. Natl Acad. Sci. USA, 76,
4932–4935.
|
|
|
|
| Arner,E.S., Bjornstedt,M. and Holmgren,A. (1995) 1-Chloro-2,4-
dinitrobenzene is an irreversible inhibitor of human thioredoxin
reductase. Loss of thioredoxin disulfide reductase activity is
accompanied by a large increase in NADPH oxidase activity. J. Biol.
Chem., 270, 3479–3482.
|
|
|
|
| the lipid analog DOPE, which differs from DPPE only by having unsaturated oleic acid in place of saturated palmitic acid and which does not partition in lipid rafts (Legler, D.F., Doucey, M.A., Cerottini, J.C., Bron, C., and Luescher, I.F. (2001). Selective inhibition of CTL activation by a dipalmitoylphospholipid that prevents the recruitment of signaling molecules to lipid rafts. FASEB J. 15, 1601–1603). 12753752
|
|
|
|
| a transfection reagent made by Roche also used for getting polyU into cells 15800576(M)
|
|
|
|
| CID: 16218742 N-(2,3-Dioleoyloxy-1-propyl)trimethylammonium methyl sulfate
|
|
|
|
| A cationic lipids known to facilitate uptake of RNA into cells 14976262(C)
|
|
|
|
| 12. Toll, L., Berzetei-Gurske, I. P., Polgar, W. E., Brandt, S. R., Adapa, I. D., Rodriguez, L., Schwartz, R. W., Haggart, D., O'Brien, A., White, A., Kennedy, J. M., Craymer, K., Farrington, L. and Auh, J. S. (1998) Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. NIDA Res Monogr, 178: 440-466. [PMID:9686407]
|
|
|
|
| a specific agonist for OpRd1 16325578(C)
|
|
|
|
| diphenylene iodonium chloride
|
|
|
|
| inhibits endothelial nitric oxide synthase
|
|
|
|
| inhibits inducible nitric oxide synthase
|
|
|
|
| inhibits mitochiodrial NADPH-ubiquinone oxido-reductase
|
|
|
|
| D-phenylalanine inhibits SLC7A5/ SLC3A2-mediated transport (Kanai et al., 1998) 19203585(C)
|
|
|
|
| Kanai, Y., Segawa, H., Miyamoto, K., Uchino, H., Takeda, E., and Endou, H. (1998). Expression cloning and characterization of a transporter for large neutral amino acids activated by the heavy chain of 4F2 antigen (CD98). J. Biol. Chem. 273, 23629–23632.
|
|
|
|
| a phospholipid that we have previously shown to partition preferentially into lipid rafts, thus selectively blocking the recruitment of the T cell receptor signaling complex to microdomains without altering their structure (Legler, D.F., Doucey, M.A., Cerottini, J.C., Bron, C., and Luescher, I.F. (2001). Selective inhibition of CTL activation by a dipalmitoylphospholipid that prevents the recruitment of signaling molecules to lipid rafts. FASEB J. 15, 1601–1603). 12753752
|
|
|
|
| dipalmitoyl phosphatidylethanolamine
|
|
|
|
| Dichlororibofuranosylbenzimidazole
|
|
|
|
| An RNA polymerase II transcriptional inhibitor. This compound terminates transcription prematurely by selective inhibition of RNA synthesis. It is used in research to study underlying mechanisms of cellular regulation
|
|
|
|
| 5,6-dichloro-1-beta-D-ribofuranosylbenose
|
|
|
|
| Casein kinase II inhibitor
|
|
|
|
| 5,6-dichloro-1-beta-D-ribofuranosyl-benzimidazole 15142038(C)
|
|
|
|
| 3,3′-Dithiodipropionic acid di(N-hydroxysuccinimide ester), DTSP, Di(N-succinimidyl) 3,3′-dithiodipropionate, Dithiobis(succinimidyl propionate), Lomant’s reagent
|
|
|
|
| Homobifunctional cross-linking reagent containing a cleavable disulfide linkage. Typically coupled to molecules containing primary amines by amide bonds buffered at pH 7.5 (6.5-8.5).
|
|
|
|
| PubChem CIDs: 446094,19001,439196
|
|
|
|
| A reagent commonly used in biochemical studies as a protective agent to prevent the oxidation of SH (thiol) groups and for reducing disulphides to dithiols.
|
|
|
|
| dynamin inhibitor 18297073(C)
|
|
|
|
| 31. Macia, E. et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev. Cell 10,
839–850 (2006).
|
|
|
|
| a lysosomal protease inhibitor 9927431(C)
|
|
|
|
| Calbiochem 324890 E-64 Protease Inhibitor
|
|
|
|
| Irreversible inhibitor of cysteine proteases. Interacts with the Sn subsites of proteases. Has no action on cysteine residues in other proteins. Inhibits activation-induced programmed cell death and restores defective immune responses in HIV+ donors. Specific active site titrant.
|
|
|
|
| essential amino acids (MEM amino acids) contains no L-Glutamine
|
|
|
|
| MW mg/L mM
L-Arginine hydrochloride 211.00 126.40 0.60
L-Cystine 240.00 24.00 0.10
L-Histidine hydrochloride-H2O 210.00 42.00 0.20
L-Isoleucine 131.00 52.40 0.40
L-Leucine 131.00 52.40 0.40
L-Lysine hydrochloride 183.00 72.50 0.40
L-Methionine 149.00 15.10 0.10
L-Phenylalanine 165.00 33.00 0.20
L-Threonine 119.00 47.60 0.40
L-Tryptophan 204.00 10.20 0.05
L-Tyrosine 181.00 36.00 0.20
L-Valine 117.00 46.80 0.40
|
|
|
|
| an analog of 1,25-dihydroxyvitamin D3 which induces a slow increased in Ca2+ , autophagy, and autophagy-dependent cell death 17244528(C)
|
|
|
|
| (2-phenyl-1,2-benzisoselenazol-3[2H]-one), a selenoorganic compound, is effective for acute ischemic stroke 14720501(C)
|
|
|
|
| A chelating agent (CHELATING AGENTS) that sequesters a variety of polyvalent cations
|
|
|
|
| peptide inhibitor PEpYINQS 21573184(M)
|
|
|
|
| peptide inhibitor PVpYHNQP 21573184(M)
|
|
|
|
| erythro-9-(2-hydroxy-3-nonyl) adenosine hydrochloride
|
|
|
|
| inhibitor of adenosine deaminase (Ada) 16497986(C)
|
|
|
|
| EgfR inhibitor 14996911(C)
|
|
|
|
| An antitumor and anti-inflammatory agent that acts as a potent, highly specific, and irreversible inhibitor of chymotrypsin-like (CT-L), trypsin-like (T-L), and peptidyl-glutamyl peptide hydrolyzing (PGPH) activities of the proteasome. Modifies the proteasomal catalytic subunits LMP-7, MECL1, and Z. Does not affect the activities of non-proteasomal proteases such as trypsin, cathepsin B, or chymotrypsin.
|
|
|
|
| SID 26758671 Calbiochem#328006
|
|
|
|
| 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione, HCl
|
|
|
|
| 17-beta-estradiol, E2 ER agonist 16143103(D)
|
|
|
|
| A semisynthetic derivative of PODOPHYLLOTOXIN that exhibits antitumor activity. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle. From: MeSH
|
|
|
|
| DNA double-strand break (DSB) inducing agent 20932476(C)
|
|
|
|
| a reagent for detecting Casp1 activation
|
|
|
|
| FMA-YVAD-FMK Caspase 1 FLICA Kit
|
|
|
|
| Immunochemistry Technologies, LLC
|
|
|
|
| a green (FAM =carboxyfluorescein) fluorescent label; an amino acid peptide inhibitor sequence targeted by active caspase 1 (YVAD); and a fluoromethylketone group (FMK) which acts as a leaving group and forms a covalent bond with the active enzyme.
|
|
|
|
| mitochondrial uncoupler 14651849(C)
|
|
|
|
| a PpaRa agonist 14525951(C)
|
|
|
|
| 5,10,15,20-tetrakis(4-sulfonatophenyl) porphyrinato iron (III)
|
|
|
|
| FeTPPS inhibits the biological effects of ONOO– by catalytically decomposing it to nitrate.
It does not interact with NO and exhibits minimal SOD mimetic activity [24].
|
|
|
|
| disrupts Lipid Rafts 15247273(C)
|
|
|
|
| Keller, P (1998) J. Cell Biol. 140, 1357–1367
|
|
|
|
| inhibits aldosterone-induced synthesis of GNAI3 [Calbio]
|
|
|
|
| inhibits FK506-binding protein -> loss of Ca2+ from SR -> decreased PP2B activity and Na+,K+-ATPase [Calbio]
|
|
|
|
| PP2B inhibitor 9880537(D)
|
|
|
|
| Fludarabine monophosphate
|
|
|
|
| irreversible inhibitor of Rsk 17360704(D)
|
|
|
|
| potently and selectively inactivates RSK1 and RSK2 in mammalian cells (Cohen et al, 2005). 16763566(C)
|
|
|
|
| Cohen MS, Zhang C, Shokat KM, Taunton J (2005) Structural bioinformatics-based design of selective, irreversible kinase in- hibitors. Science 308: 1318–1321
|
|
|
|
| activates adenyl cyclases at 4 uM
|
|
|
|
| increases cyclic-AMP levels
|
|
|
|
| a 45-kDa noncatalytic peptide of FAK that contains Ser732 (Parsons, 2003)
|
|
|
|
| Parsons, J. T. (2003). Focal adhesion kinase: the first ten years. J. Cell Sci. 116, 1409 –1416.
|
|
|
|
| farnesyl transferase inhibitor 12842888(C)
|
|
|
|
| binds PIP3, used as marker for early endosomes 14716310(C)
|
|
|
|
| However, we found that high level expression of the 2X-FYVE domain leads to sequestration of PI(3)P and disruption of PI(3)P-dependent signaling, as indicated by the loss of EEA1 endosomal targeting. `
|
|
|
|
| such vectors are known to function as dominant interfering
proteins, by competing for intracellular PI3P-docking sites.
|
|
|
|
| aka Iressa an anti-EgfR agent 15950906(C)
|
|
|
|
| Hsp90 inhibitor 11779866(C)
|
|
|
|
| an ansamycin antibiotic that inhibits Hsp90 function, 15001580(C)
|
|
|
|
| Certain ansamycin antibiotics, such as geldanamycin, occupy
the ATP/ADP binding pocket of Hsp90 to inhibit its chaperone
activities (23, 24) and, as such, often decrease the cellular
levels of Hsp90 client proteins. 15001580(C)
|
|
|
|
| 23. Stebbins, C. E., Russo, A. A., Schneider, C., Rosen, N., Hartl, F. U., and
Pavletich, N. P. (1997) Cell 89, 239 –250
24. Roe, S. M., Prodromou, C., O’Brien, R., Ladbury, J. E., Piper, P. W., and Pearl,
L.H. (1999) J. Med. Chem. 42, 260–266
|
|
|
|
| GA was previously shown to interact and interfere with the normal functions of Hsp90 (Whitesell et al., 1994). 11864612(C)
|
|
|
|
| Ppara agonist 11009565(C)
|
|
|
|
| tyrosine kinase inhibitor 15485651(C)
|
|
|
|
| usually refers to L-Glutamine or a mix of L-Glutamine and D-Glutamine
|
|
|
|
| a raft-associated lipid detected using Cy5-cholera toxin 16880211(C)
|
|
|
|
| Monosialoganglioside GM3 ALX-302-005
|
|
|
|
| [II3Neu5AcLacCer] [α-Neu5Ac-(2→3)]-β-Gal(1→4)-β-Glc-(1→1')-Cer]
|
|
|
|
| Inhibits PKCa PKCb PKCm 11278339(D)
|
|
|
|
| PKCa specific inhibitor 1134345(C)
|
|
|
|
| Inhibits PKCa PKCb PKCg PKCd PKCz 11278339-D
|
|
|
|
| L-g-glutamyl-p-nitroanilide, an inhibitor of SLC1A5- regulated transport (Esslinger et al., 2005) 19203585(C)
|
|
|
|
| Esslinger, C.S., Cybulski, K.A., and Rhoderick, J.F. (2005). Ngamma-aryl glutamine analogues as probes of the ASCT2 neutral amino acid transporter binding site. Bioorg. Med. Chem. 13, 1111–1118.
|
|
|
|
| A sulfur-containing alkyl thionitrite that is one of the NITRIC OXIDE DONORS CID 3514
|
|
|
|
| Calbiochem #361540 GSK-3β Inhibitor I
|
|
|
|
| A thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP competitive inhibitor of GSK-3β (IC50 = 2 μM). Inhibits Flt-3 and PKC activities (IC50 = 673 nM and 1.4-5.5 μM, respectively). Does not significantly affect the activities of Cdk-1/cyclin B, CK-II, and PKA, (IC50 > 100 μM). Binds to the active site of GSK-3β.
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| Calbiochem 361541 GSK-3b Inhibitor II
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| 2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole
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| A 2-thio-[1,3,4]-oxadiazole-pyridyl derivative that acts as a potent inhibitor of glycogen synthase kinase-3β (IC50 = 390 nM).
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| Calbiochem #361550 BIO, (2′Z,3′E)-6-Bromoindirubin-3′-oxime
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| A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3α/β (IC50 = 5 nM). Its specificity has been tested against various Cdk's (IC50 = 83, 300, 320, and 10,000 nM for Cdk5/p25, Cdk2/A, Cdk1/B, and Cdk4/D1, respectively) as well as many other commonly studied kinases (IC50 ≥ 10 µM), including MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK. Inhibition of GSK by BIO has been shown to result in the activation of Wnt-signaling pathway and sustained pluripotency in human and murine ESCs (embryonic stem cells). Reported to maintain self-renewal in human and mouse embryonic stem cells. Also induces the differentiation of neonatal cardiomyocytes.
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| Calbiochem #361553 GSK-3β Inhibitor XI
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| 3-(1-(3-Hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-pyrazin-2-yl-pyrrole-2,5-dione, 7AIPM
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| A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 25 nM) and minimally inhibits a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells with an EC50 of 32 nM and demonstrate metabolic stability in human liver microsomes (HLM; t1/2 > 100 min).
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| LxRa/b agonist 16143103(C)
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| PpaRd agonist 14525954(C)
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| a specific inhibitor of Raf1 16806820(C)
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| PpaRg agonist 16143103(C)
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| 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine 9305919(C)
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| serine/threonine kinase inhibitor 9305919(C)
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| 24. Zhang, X., Blenis, J., Li, H.-C., Schindler, C., and Chen-Kiang, S. (1995)Science 267, 1990–1994
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| inhibitor of PKA PKG PKC from Calbiochem 12150925(C)
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| Src inhibitor 11907028(C)
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| Humanized monoclonal antibody to ErbB2 gamma1-chain
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| human-mouse monoclonal rhuMab HER2 gamma1-chain, disulfide with human mouse monoclonal rhuMab
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| Trastuzumab, Trastuzumab [INN]
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| Immunoglobulin G1, anti-(human p185neu receptor
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| An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. From: MeSH
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| Polycyclic dione that has anti-retroviral activity. Inhibits protein kinase C (IC50 = 3.3 mM). Also known to inhibit casein kinase II (IC50 = 6 nM), MAP kinase (IC50 = 4 nM), and the protein tyrosine activities of the insulin receptor (IC50 = 20 - 29 nM) and the epidermal growth factor receptor (IC50 = 35 nM). Purity: ≥95% by HPLC. CAS 548-04-9.
Merck Index: 14, 4863
Ref.: Zhang, W., et al. 1997. Cancer Lett. 120, 31. Agostinis, P., et al. 1995. Biochem. Pharmacol. 49, 1615. Frew, T., et al. 1994. Anticancer Res. 14, 2425. Barnard, D.L., et al. 1992. Antiviral Res. 17, 63. Takahashi, I., et al. 1989. Biochem. Biophys. Res. Commun. 165, 1207.
R: 22; S: 22-36
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| 3-isobutyl-1-methylxanthine
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| Inhibits cAMP and cGMP phosphodiesterases which causes increase in cAMP and PKA-act
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| phosphodiesterase inhibitor 11292821(C)
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| thromboxane A2/prostaglandin H2 receptor agonist
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| 7-(3-(3-hydroxy-4-(4'-iodophenoxy)-1-butenyl)-7-oxabicyclo(2.2.1)heptan-2-yl)-5-heptenoic acid
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| Calbiochem 400090 3-[(2,4,6-Trimethoxyphenyl)methylidenyl]-indolin-2-one, SU5607
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| cell-permeable, reversible, potent and selective inhibitor of casein kinase (CK1) that inhibits CK1δ (IC50 = 0.7-1.3 µM) and CK1ε (IC50 = 0.6-1.4 µM) isozymes. Also inhibits CK1α1 at much higher concentrations (IC50 = 11-21 µM). The inhibition is competitive with respect to ATP. Only weakly inhibits PKA, p34cdc2, and p55fyn (IC50s > 100 µM). At low micromolar concentrations, IC261 inhibits cytokinesis causing a transient mitotic arrest.
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| a specific inhibitor of CK1 (24) 18067272(C)
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| 24. Holler, N., Zaru, R., Micheau, O., Thome, M., Attinger, A., Valitutti, S., Bodmer, J. L., Schneider, P., Seed, B., and Tschopp, J. (2000) Fas triggers an alternative, caspase-8-independent cell death pathway using the kinase RIP as effector molecule, Nat. Immunol. 1, 489-495.
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| Z-Ile-Glu(OtBu)-Ala-Leu-H
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| [PSI] Benzyloxycarbonyl-L-Isoleucyl-[(2S)2-Amino-4-(t-Butyloxycarbonyl)Butanoyl]-L-Alanyl-L-Leucinal (M.W. 618.76) C32H50N4O8 [158442-41-2] Synthetic Product Inhibitor for Proteasome M.E. Figueiredo-Pereira, K.A. Berg, and S. Wilk, J. Neurochem., 63, 1578 (1994). E.B.-M. Traenckner, S. Wilk, and P.A. Baeuerle, EMBO J., 13, 5433 (1994). M.E. Figueiredo-Pereira, W-E. Chen, H-M. Yuan, and S. Wilk, Arch. Biochem. Biophys., 317, 69 (1995).
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| [5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
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| A cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
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| cyclooxygenase inhibitor [7592593]
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| a cyclooxygenase-1/cyclooxygenase-2 inhibitor [17277110]
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| a Ca2+ ionophore that serves as a mobile Ca2+ carrier that equilibrates Ca2+ levels across biological membranes, including plasma and ER membranes 17244528(C)
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| inositol 1,4,5-trisphosphate
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| 2-methylpropan-1-ol, isobutyl alcohol
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| AdRb2 agonist 12082090(C)
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| Inhibits both Jak1 and Jak3 17200144(C)
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| Cramer, L. P. (1999). Role of actin-filament disassembly in lamellipodiumprotrusion in motile cells revealed using the drug jasplakinolide. Curr. Bio9, 1095-1105.
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| Inhinits actin disassemly?
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| a cell permeable peptide inhibitor from Calbiochem 12738796(C)
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| metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor
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| staurosporinone
k-252a
k-252b
K252a
3'-(S)-epi-K-252a
K 252a
K 252b
K 252c
K 252d
K-252c
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| Potassium Dichromate 19276070(C)
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| Kaede is a recently cloned f luorescent protein that emits bright green fluorescence after its synthesis, which changes efficiently to a stable red fluorescence upon irradiation with 405-nm light, thereby providing a simple and powerful technique for the regional optical labeling of target molecules.
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| 22. Ando R, Hama H, Yamamoto-Hino M, Mizuno H, Miyawaki A (2002) Proc Natl Acad Sci USA 99:12651–12656.
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| a Rsk2 inhibitor 20385620(C)
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| 29. Cho, Y. Y., Yao, K., Kim, H. G., Kang, B. S., Zheng, D., Bode, A. M., and Dong, Z. (2007) Ribosomal S6 kinase 2 is a key regulator in tumor promoter induced cell transformation. Can-
cer Res. 67, 8104 – 8112
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| Kainate, a model excitotoxin, activates both AMPA and kainate receptor subtypes and can induce seizures and hippocampal neuronal apoptosis in vivo (Ferkany et al., 1984; Pollard et al., 1994; Schreiber et al., 1993) as well as trigger cell death in cultured primary neurons (Koh et al., 1990). 12194869(C)
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| 39. Leclerc, S., Garnier, M., Hoessel, R., Marko, D., Bibb, J. A., Snyder, G. L.,
Greengard, P., Biernat, J., Wu, Y. Z., Mandelkow, E. M., Eisenbrand, G.,
and Meijer, L. (2001) J. Biol. Chem. 276, 251–260
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| alpha-ketoisocaproic acid
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| production of glutamate from alpha-ketoglutarate during transamination of leucine to alpha-ketoisocaproic acid [6800820] 17287212(C)
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| antagonist of P2X7 receptor 16497986(C)
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| Camk2 inhibitor 16497986(C)
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| 1-[N,O-bis(5-iso-quinolinesulphonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine
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| inhibits Camk2 11397791(C)
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| Ilk inhibitor KP-SD-1 11313365(C)
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| Atm kinase inhibitor 209324176(C)
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| Hickson, I., Zhao, Y., Richardson, C.J., Green, S.J., Martin, N.M., Orr, A.I., Reaper, P.M., Jackson, S.P., Curtin, N.J., and Smith, G.C. (2004). Identification and characterization of a novel and specific inhibitor of the ataxia-telangi- ectasia mutated kinase ATM. Cancer Res. 64, 9152–9159.
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| 17446862(C) autophagy producer
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| Calbiochem 426100 Lactacystin, Synthetic
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| An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM).
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| proteasome inhibitor 11684013(C)
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| 26S proteasome inhibitor 10587642(C)
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| irreversible proteasome inhibitor 16467847(C)
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| Lambda Protein Phosphatase NEN#P0753
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| Lambda Protein Phosphatase (Lambda PP) is a Mn2+-dependent protein phosphatase with activity towards phosphorylated serine, threonine and tyrosine residues. It is the 221 amino-acid product of the ORF221 open reading frame on bacteriophage lambda (1,2).
|
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|
|
| 1. Cohen, P.T.W. and Cohen, P. (1989) Biochem. J., 260, 931-934.
2. Zhuo, S. et al. (1993) J. Biol. Chem., 268, 17754-17761.
3. Gordon, J.A. (1991) Methods Enzymol., 201, 477-482.
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| an inhibitor of actin assembly
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| blocks phagocytosis by stablizing actin 15711573(C)
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| The latrunculins are commonly used to experimentally disrupt the actin cytoskeleton of cells. Latrunculin B causes concentration-dependent changes in cell shape and actin organization. It sequesters G-actin and prevents F-actin assembly. It binds monomeric actin with 1:1 stoichiometry and can be used to block actin polymerization both in vitro and in cells (Kd = 60 nM).1 The short-term effects of latrunculin B are comparable to those of latrunculin A, although latrunculin B is slightly less potent.2 However, latrunculin B is gradually inactivated by serum so that induced changes are transient in the continued presence of the compound. For this reason, latrunculin B may have fewer unwanted effects than latrunculin A and may be preferred for short-term studies.
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|
| Spector, I., Schochet, N.R., Blasberger, D., et al. Latrunculins-novel marine macrolides that disrupt microfilament organization and affect cell growth: I. comparison with cytochalasin D. Cell Motil Cytoskeleton 13 127-144 (1989).
Wakatsuki, T., Schwab, B., Thompson, N.C., et al. Effects of cytochalasin D and latrunculin B on mechanical properties of cells. J Cell Sci 114 1025-1036 (2000).
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|
| Structurally unique marine toxin. Actin filament modulator. 10- to 100-fold more potent than cytochalasins. Whereas cytochalasin D induces dissolution of F-actin and stress fiber contraction in fibroblasts in culture, latrunculin B causes a shortening and thickening of stress fibers. Effects on N1E-115 cells (mouse neuroblastoma) at concentrations as low as 90nM (NI43T3 cells, 0.9μM). Maximum effects at 2.5μM. Slowly inactivated by fetal bovine serum. Inhibition of cofilin-actin binding (ED50~50µM)
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| Btk inhibitor 15849198(C) 16415872(C)
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| a synthetic RXR agonist 14525954(C)
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| Inhibits GSK3 11147790(D)
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| acts as a potent inhibitor of both mammalian GSK-3 isoforms (32) 14563837(C)
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| 23. Lutterbach, B., and Hann, S. R. (1994) Mol. Cell. Biol. 14, 5510–5522
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|
| is a lipid component of an endotoxin held responsible for toxicity of Gram-negative bacteria. It is the innermost of the three regions of the lipopolysaccharide (LPS, also called endotoxin) molecule, and its hydrophobic nature allows it to anchor the LPS to the outer membrane. [Wikipedia]
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|
| Z-Leu-Leu-Leu-H (aldehyde)
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|
|
| Benzyloxycarbonyl-L-Leucyl-L-Leucyl-L-Leucinal (M.W. 475.62) C26H41N3O5 [133407-82-6] Synthetic Product Inhibitor for Proteasome and Cathepsin K Y. Saito, S. Tsubuki, H. Ito, and S. Kawashima, Neurosci. Lett., 120, 1 (1990). T.J. Jensen, M.A. Loo, S. Pind, D.B. Williams, A.L. Goldberg, and J.R. Riordan, Cell, 83, 129 (1995). B.J. Votta, M.A. Levy, A. Badger, J. Bradbeer, R.A. Dodds, I.E. James, S. Thompson, M.J.Bossard, T. Carr, J.R. Conner, T.A. Tomaszek, L. Szewczuk, F.H. Drake, D.F. Veber, and M. Gowen, J. Bone Miner. Res., 12, 1396 (1997) • This compound is distributed through Peptide Institute, Inc. under the license of Dr. H. Ito.
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| Z-Leu-Leu-Nva-H (aldehyde)
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| [MG-115] Benzyloxycarbonyl-L-Leucyl-L-Leucyl-L-Norvalinal (M.W. 461.59) C25H39N3O5 [133407-86-0] Synthetic Product Inhibitor for Proteasome Y. Saito, S. Tsubuki, H. Ito, and S. Kawashima, Neurosci. Lett., 120, 1 (1990). A. Vinitsky, C. Michaud, J.C. Powers, and M. Orlowski, Biochemistry, 31, 9421 (1992). K.L. Rock, C. Gramm, L. Rothstein, K. Clark, R. Stein, L. Dick, D. Hwang, and A.L. Goldberg, Cell, 78, 761 (1994). V.J. Palombella, O.J. Rando, A.L. Goldberg, and T. Maniatis, Cell, 78, 773 (1994). • This compound is distributed through Peptide Institute, Inc. under the license of Dr. H. Ito.
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|
| an inhibitor of Crml nuclear export pathway 16624523(C)
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| a specific inhibitor of NES-dependent intracellular transport 11265759(C)
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|
| a specfic inhibitor for Crm1 (Xpo1)
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|
| 17. Fornerod, M., M. Ohno, M. Yoshida, and I. W. Mattaj. 1997. CRM1 is an
export receptor for leucine-rich nuclear export signals. Cell 90:1051–1060.
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| 39. Ossareh-Nazari, B., F. Bachelerie, and C. Dargemont. 1997. Evidence for a
role of CRM1 in signal-mediated nuclear protein export. Science 278:141–
144.
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|
| L-N6-iminoethyl-lysine (L-NIL), a potent competitive inhibitor of NOS2 (9) 10320373(C)
|
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|
| A. Diefenbach et al., Immunity 8, 77 (1998)
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|
| Lipoteichoic acid, Teichoic acid
|
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|
|
| lipopolysaccharides with an acyl group anchored to the cell membrane of gram-positive bacteria; functions as an adhesion molecule to facilitate the binding of bacteria to cells, colonization, and invasion; interacts with CD14 to induce NF-kB activation and inflammatory cytokine production; can function as surface antigen
|
|
|
|
| Inhibits Pi3k 16497986(C)
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|
| 2-(4-Morpholinyl)-8- phenyl-1(4H)-benzopyran-4-one hydrochloride
|
|
|
|
| a shellfish toxin 17186029(C)
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|
|
| blocks caspase-1 activation, IL1b release, IL18 release irt TLR stimulation 16407890(D)
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|
| thiol modifying agent 15896328
|
|
|
|
| F. Tewes, G.F. Bol, R. Brigelius-Flohe, Thiol modulation inhibits the interleukin (IL)-1-mediated activation of an IL-1 receptor-associated protein kinase and NF-kappa B, Eur. J. Immunol. 27
(1997) 3015–3021.
|
|
|
|
| A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)
|
|
|
|
| disrupts cholesterol 12717440(C)
|
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|
|
| Simons,K.& Toomre,D.Lipid rafts and signal transduction.Nature Rev. Mol. Cell Biol. , 31–39 (2000).
|
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|
| 15793306: therefore relevant to note that in several tumor cell lines,
which may or may not form caveolae, disruption of lipid rafts by extraction of cholesterol with methyl-beta-cyclodextrin can reduce Nfkb activation [15].
|
|
|
|
| 15. Legler DF, Micheau O, Doucey MA, Tschopp J, Bron C: Recruitment
of TNF receptor 1 to lipid rafts is essential for TNFalpha-mediated
NF-kappaB activation. Immunity 2003, 18:655– 664
|
|
|
|
| 15175328(C): disrupts lipid rafts
|
|
|
|
| disrupts lipid rafts by specific cholesterol depletion [Harder, T., Scheiffele, P., Verkade, P., and Simons, K. (1998). Lipid domain structure of the plasma membrane revealed by patching of membrane components. J. Cell Biol. 141, 929–942.
Janes, P.W., Ley, S.C., and Magee, A.I. (1999). Aggregation of lipid rafts accompanies signaling via the T cell antigen receptor. J. Cell Biol. 147, 447–461.]
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| 14713952(C): depletes cholesterol
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| a growth factor-independent energy source 17237771(C)
|
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|
|
| 24 h following transfection, cells were serum-starved for 16 h in serum-free medium containing 4 mM mevalonolactone (COS-1 cells do not contain sufficient amounts of endogenous isoprenoid precursors to farnesylate overexpressed Ras proteins, so medium was supplemented with mevalonolactone to augment available precursors). 10358073(C)
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|
| 26S Proteasome inhibitor 10587642(C)
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|
|
| 10.Rock, K. L. et al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell 78, 761–771 (1994).
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| Zlllal
Z-Leu-Leu-Leu-H
zLLL
Z-Leu-leu-leu-al
nchembio790-comp6
Cbz-Leu-Leu-Leu-H N-CBZ-Leu-Leu-Leu-al
nchembio.130-comp1
Z-LLL-CHO
MG132
BSPBio_001310
KBioGR_000030
KBioSS_000030
C2211_SIGMA
NChemBio.2007.18-comp4
BCBcMAP01_000028
KBio2_000030
KBio2_002598
KBio2_005166
KBio3_000059
KBio3_000060
CHEBI:199755
MG-132
AIDS031965
Bio2_000030
Bio2_000510
AIDS-031965
CID462382
ZINC13476439
Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal
IDI1_033780
NCGC00161679-01
NCGC00161679-02
NCGC00161679-03
UNM000011053701
SR-01000864598-1
BRD-K60230970-001-04-3
L-Leucinamide, N-[(phenylmethoxy)carbonyl]-L-leucyl-N1-[(1S)-1-formyl-3-methylbutyl]-
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
{(S)-1-[(S)-1-((S)-1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester
{1-[(S)-(S)-1-((S)-1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester
{1-[1-(1-Formyl-3-methyl-butylcarbamoyl)-3-methyl-butylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl ester
133407-82-6
benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate
Benzyl N-[(1S)-3-methyl-1-[[(1S)-3-methyl-1-[[(2S)-4-methyl-1-oxo-pentan-2-yl]carbamoyl]butyl]carbamoyl]butyl]carbamate
|
|
|
|
| Zillal
Zlll-cho
Lll cpd
Z-Leu-leu-leu-al
Z-Leu-leu-leucinal
Z-LLL
Carbobenzoxy-leucyl-leucyl-leucinal
CHEBI:476512
MG 132
Benzyloxycarbonyl-leu-leu-leu-aldehyde
C26H41N3O5
MG132
Benzyloxycarbonyl-leucyl-leucyl-leucinal
CID107707
MG-132
Carbobenzoxyl-leucinyl-leucinyl-leucinal-H
carbobenzyloxy-leucinyl-leucinyl-leucinal
Benzyloxycarbonylleucyl-leucyl-leucine aldehyde
LS-172868
(S)-N-((Phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-3-methylbutyl)-L-leucinamide
L-Leucinamide, N-((phenylmethoxy)carbonyl)-L-leucyl-N-((1S)-1-formyl-3-methylbutyl)-
L-Leucinamide, N-((phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-3-methylbutyl)-, (S)-
133407-82-6
benzyl 4-methyl-1-(4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate
|
|
|
|
| a proteasome inhibitor 10713156(C)
|
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|
|
| ML-7 a MLCK (Mylk) inhibitor 14747473(C)
|
|
|
|
| myosin light chain from various species used as a substrate for Rock1
|
|
|
|
| competitive inhibitor of Prolyl-hydroxylases
|
|
|
|
| dimethyloxalylglycine - an ester of N-oxalylglycine that penetrates cells
|
|
|
|
| an alkylating agent 12110590(C) 7737130(C)
|
|
|
|
| an inducer of JnkS and P38S 12110590(C)
|
|
|
|
| N-methyl-N'-nitro-N-nitroso-guanidine
|
|
|
|
| an alkylating compound 7737130(C)
|
|
|
|
| inhibites transport of proteins from Golgi apparatus 11163183(C)
|
|
|
|
| Uchida, N., Smilowitz, H., Ledger, P.W., and Tanzer, M.L. (1980). Kinetic studies of the intracellular transport of procollagen and fibronectin in human fibroblasts. Effects of the monovalent ionophore, monensin. J. Biol. Chem. 255, 8638–8644.
|
|
|
|
| Monodansylcadaverine (a primary amine 10187805(C))
|
|
|
|
| marker for autophagic vacuoles [7750517] 15607973(C)
|
|
|
|
| 10187805(C): MDC is an inhibitor of transglutaminase, a membrane-bound
enzyme that actively participates in internalization of various
receptor systems (36 – 44).
|
|
|
|
| 36. Folk, J. E., and Chung, S. H. (1973) Adv. Enzymol. 38, 109 –191
|
|
|
|
| 37. Davies, P., Davis, D., Levitzki, F., Maxfield, P., Milhaud, M., Willingham, C., and Pastan, I. (1980) Nature 283, 162–167
|
|
|
|
| 38. Chow, J. C., Condorelli, G., and Smith, R. J. (1998) J. Biol. Chem 273,
4672– 4680
|
|
|
|
| 39. Resink, T. J., Scott Burden, T., Boulanger, C., Weber, E., and Buhler, F. R. (1990) Mol. Pharmacol. 38, 244 –252
|
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|
| 40. Samanta, A. K., Oppenheim, J. J., and Matsushima, K. (1990) J. Biol. Chem. 265, 183–189
|
|
|
|
| 41. Bradley, J. R., Johnson, D. R., and Pober, J. S. (1993) J. Immunol. 12,
5544 –5555
|
|
|
|
| 42. Peavy, D. E., Edmondson, J. W., and Duckworth, W. C. (1984) Endocrinology 114, 753–760
|
|
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|
| 43. Ray, E., and Samanta, A. K. (1996) FEBS Lett. 378, 235–239
|
|
|
|
| 44. Ray, E., and Samanta, A. K. (1997) Cytokine 9, 587–596
|
|
|
|
| a "danger signal" 17599095(C)
|
|
|
|
| a peptide derived from the protein kinase inhibitor (PKI), myristoylated PKI 14-22 amide
(myr-PKI; #476485), was from Calbiochem. 16581779(C)
|
|
|
|
| inhibitor of mitochondrial respiration 16565215(C)
|
|
|
|
| N6-Methyl-2-deoxyadenosine
|
|
|
|
| methylation inhibitor 15153491(C)
|
|
|
|
| PubChem CIDs: 12035,94364
|
|
|
|
| The N-acetyl derivative of CYSTEINE. It is used as a mucolytic agent to reduce the viscosity of mucous secretions. It has also been shown to have antiviral effects in patients with HIV due to inhibition of viral stimulation by reactive oxygen intermediates.
|
|
|
|
| 9564042(C): a thiol-based redox compound, Nac, which is also a potent antioxidant.
|
|
|
|
| peptide derived from the Nemo Binding Domain of Ikk2 14651848(C)
|
|
|
|
| May, M.J., D’Acquisto, F., Madge, L.A., Glockner, J., Pober, J.S., and Ghosh, S. (2000). Selective inhibiton of NF-kB activation by a peptide that blocks the interaction of NEMO with the IkB kinase complex. Science 289, 1550–1554.
|
|
|
|
| drqikiwfqnrrmkwkkTALDWSWLQTE
|
|
|
|
| inhibitor of Slc29a1 16497986(C)
|
|
|
|
| NCS belongs to a family of enediyne antibiotics that intercalate into the DNA and induce double-strand breaks by free radical attack on the deoxyribose moieties in both DNA strands. The biological effects of these compounds are similar to those of ionizing radiation (19). 9733514(C)
|
|
|
|
| 19. I. H. Goldberg and L. S. Kappen, in Enediyne Antibiotics as Antitumor Agents, D. B. Borders and T. W. Doyle, Eds. (Dekker, New York, 1995), pp. 327–362.
|
|
|
|
| Like IR, NCS induces DNA double-strand breaks by free radical attack and elicits the same hypersensitivity of A-T cells (38).
|
|
|
|
| 38. I. H. Goldberg and L. S. Kappen, in Enediyne Antibiotics as Antitumor Agents, D. B. Borders and T. W. Doyle, Eds. (Dekker, New York, 1995), pp. 327–362.
|
|
|
|
| a drug that generates a high yield of DNA DSBs 16327781(C)
|
|
|
|
| 22.D’Andrea,A.D.&Haseltine,W.A. Sequence specific cleavage of DNA by the antitumor
antibiotics neocarzinostatin and bleomycin. Proc. Natl Acad. Sci. USA 75, 3608–3612
(1978).
|
|
|
|
| lipooxygenase inhibitor [7592593]
|
|
|
|
| nordihydroguaiaretic acid
|
|
|
|
| Non-essential amino acids
|
|
|
|
| A sulfhydryl reagent that is widely used in experimental biochemical studies.
|
|
|
|
| N-ethylmaleimide; Ethylmaleimide
|
|
|
|
| N-Ethylmaleimide (NEM) is a chemical derivative of maleic acid imide or maleic acid. It is a thiol reactive compound commonly used to modify cystine residues in proteins and peptides.
|
|
|
|
| It can be used to irreversibly inhibit the formation of cystine linking in proteins
|
|
|
|
| It has been observed that after addition of NEM vesicular transport was blocked. After identification of the responsible protein it was called N-ethylmaleimide-sensitive factor (NSF).
|
|
|
|
| In lysis buffers, 20 to 25 mM of NEM is used to inhibit de-sumoylation of proteins for Western Blot analysis.
|
|
|
|
| NEM is also used as an inhibitor of deubiquitinases.
|
|
|
|
| inhibits Ca2 uptake through L-type channels 11463795(C)
|
|
|
|
| A bacterial derived potassium ionophore 17186029(C)
|
|
|
|
| blocks caspase-1 activation, IL1b release, IL18 release irt TLR stimulation 16407890(D)
|
|
|
|
| nucleoside transport inhibitor [2866831] 14978242(C)
|
|
|
|
| 4-Hydroxy-5-iodo-3-nitrophenylacetyl-Leu-Leu-Leu-vinylsulfone, NIP-L3VS
|
|
|
|
| An irreversible proteasome inhibitor that inhibits trypsin-like and chymotrypsin-like activities in isolated proteasomes, and blocks their function in living cells. In contrast to Lactacystin, it also inhibits the peptidyl-glutamyl peptidase activity of proteasomes. Covalently modifies the active site threonine of the catalytic β-subunit of the proteasome.
|
|
|
|
| A competitive inhibitor of nitric oxide synthetase PubChem CID 135424
|
|
|
|
| Promotes tubulin depolymerization (CalBio)
|
|
|
|
| Nocodazole is an antineoplastic agent which exerts its effect by depolymerizing microtubules.
|
|
|
|
| competitive inhibitor of Prolyl-hydroxylases
|
|
|
|
| IUPAC Name: 2-(carboxymethylamino)-2-oxo-acetic acid
|
|
|
|
| aka: NU7026, NU 7026, LY-293646, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, DNA-PK Inhibitor II, CHEMBL104468, CHEBI:270938, HMS3229C11, DNC000625
|
|
|
|
| a DNA-PK inhibitor 18006705(C)
|
|
|
|
| a small molecule that blocks the binding of HDM2 to p53 15029243(C)
|
|
|
|
| Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, Kong N, Kammlott U, Lukacs C, Klein C, Fotouhi N, Liu EA (2004) In vivo activation of the p53 pathway by small-molecule antago- nists of MDM2. Science 303: 844–848
|
|
|
|
| disrupts Lipid Rafts 15247273(C)
|
|
|
|
| Anderson, HA (1996) Mol. Biol. Cell 7, 1825–1834
|
|
|
|
| disrupts cholesterol 12717440(C)
|
|
|
|
| Simons,K.& Toomre,D.Lipid rafts and signal transduction.Nature Rev. Mol. Cell Biol. , 31–39 (2000).
|
|
|
|
| Inhibits PP2A cataylic subunit not acid or alkaline phosphatases, or PTPases [2539153]
|
|
|
|
| Okadaic acid inhibits PP2A at concentrations up to 1 M without inhibiting PP1 [10692405] 11292821(C)
|
|
|
|
| an inhibitor of the PP2A family 17079228(C)
|
|
|
|
| inhibitor of oxidative phosphorylation
|
|
|
|
| inhibitor of the mitochondrial F0F1-AT P synthase
|
|
|
|
| Tyrosine phosphatase inhibitor
|
|
|
|
| borellia burgdorferii lipoprotein a TLR2 ligand 11896392(C)
|
|
|
|
| inhibits the sodium pump and blocks the sodium pump component of oxidative phosphorylation and reduces basal oxygen consumption
|
|
|
|
| chick ovalbumin peptide (amino acids 323 through 339)
|
|
|
|
| viral caspase inhibitor 11262391(M)
|
|
|
|
| aka Pam3Cys or BLP - bacterial lipopeptide 12447442(C)
|
|
|
|
| 18. Takeuchi, O. et al. Cutting edge: role of toll-like receptor 1 in mediating immune response to microbial lipoproteins. J. Immunol. 169, 10–14 (2002).
|
|
|
|
| N-palmitoyl-S-dipalmitoylglyceryl (Pam3) Cys-Scr-(Lys)4 (CSK4)
|
|
|
|
| A membrane-permeable protein tyrosine phosphatase inhibitor (IC50 = 18 µM). Stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle and activates p56lck protein tyrosine kinase. Blocks TNF-α-dependent activation of NF-κB in human myeloid ML-1a cells. PAO inhibits the protease activities of recombinant human caspases as well as endogenous caspases that are active in extracts of pre-apoptotic chicken DU249 cells (S/M extracts).
|
|
|
|
| Phenylarsine oxide inhibits internalization of cell surface receptors; inhibits tyrosine phosphatases, with no effect on tyrosine kinase. Metabolic poison.
|
|
|
|
| inhibitor of protein tyrosine phosphatases (PTPases) previously shown to be selective in preventing dephosphorylation of FAK and paxillin
10655584(D)33,34.
|
|
|
|
| 33.Retta, S. F. et al. Focal adhesion and stress fiber formation is regulated by tyrosine phosphatase activity. Exp. Cell Res. 229, 307–317 (1996).
34.Defilippi, P. et al. p125FAK tyrosine phosphorylation and focal adhesion assembly: studies with phosphotyrosine phosphatase inhibitors. Exp. Cell Res. 221, 141–152 (1995).
|
|
|
|
| inhibitor of endocyctosis 12093727(C)
|
|
|
|
| Hertel,C., Coulter,S.J. and Perkins,J.P. (1985) A comparison of catecholamine-induced internalization of b-adrenergic receptors and receptor-mediated endocytosis of epidermal growth factor in human astrocytoma cells. Inhibition by phenylarsine oxide. J. Biol. Chem., 260, 12547±12553.
|
|
|
|
| Tong,X.K., Hussain,N.K., Adams,A.G., O'Bryan,J.P. and McPherson,P.S. (2000) Intersectin can regulate the Ras/MAP kinase pathway independent of its role in endocytosis. J. Biol. Chem., 275, 29894-29899.
|
|
|
|
| 10938077(C) PD144795 is a benzothiophene, which was originally found to inhibit HIV expression (50)
|
|
|
|
| 50. Critchfield, J. W., Butera, S. T., and Folks, T. M. (1996) AIDS Res. Hum. Retroviruses 12, 39 – 46
|
|
|
|
| aka AG1517, Compound 32, SU5271
|
|
|
|
| EGFR kinase IC50=25pM Ki=6pM (CalBio)
|
|
|
|
| inhibits EGFR kinase activity 12952935(D)
|
|
|
|
| EgfR kinase inhibitor 15950906(C)
|
|
|
|
| P38 MAPK inhibitor 15326485(C)
|
|
|
|
| Calbiochem #513030 PD 169316
|
|
|
|
| 4-(4-Fluorophenyl)-2-(4-nitrophenyl)-5-(4-pyridyl)-1H-imidazole
|
|
|
|
| A potent, cell-permeable, and selective p38 MAP kinase inhibitor (IC50 = 89 nM). Inhibition of p38 MAP kinase by PD 169316 blocks apoptosis induced by trophic factor withdrawal in non-neuronal and neuronal cell lines.
|
|
|
|
| PD 184352 is a potent and specific inhibitor of MAPK kinase 1, the enzyme that activates ERK1 and ERK2) [24] 15304344(C)
|
|
|
|
| [24] Sebolt-Leopold, J.S., Dudley, D.T., Herrera, R., Van Becelaere, K., Wiland, A., Gowan, R.C., Tecle, H., Barrett, S.D., Bridges, A., Przybranowski, S., Leopold, W.R. and Saltiel, A.R. (1999) Nat. Med. 5, 810–816.
|
|
|
|
| a Mek inhibitor supplied by Pfizer 19953085(C)
|
|
|
|
| activates PKC 11283245(C)
|
|
|
|
| activates PKD 11784866(C)
|
|
|
|
| Phosphatidylethanolamine, cephalin
|
|
|
|
| a lysosomal protease inhibitor 16874098(C)
|
|
|
|
| A reversible inhibitor of aspartic proteases. Inhibits cathepsin D, pepsin, renin [Calbio]
|
|
|
|
| A potent oxidant synthesized by the cell during its normal metabolism. Peroxynitrite is formed from the reaction of two free radicals, NITRIC OXIDE and the superoxide anion (SUPEROXIDES)
|
|
|
|
| H2O2 + orthovanadate 10187801(C)
|
|
|
|
| Met inhibitor 19274086(C)
|
|
|
|
| used as a P38 inhbitor in 19953085 as a gift from Pfizer
|
|
|
|
| no other information supplied
|
|
|
|
| a biguanide widely used to treat type 2 diabetes 17287212(C)
|
|
|
|
| a radio-mimetic drug 18006705(C)
|
|
|
|
| a Pi3k inhibitor that also inhibits MTorc1 and Mtorc2 18925875(C)
|
|
|
|
| 45 Raynaud, F. I., Eccles, S., Clarke, P. A., Hayes, A., Nutley, B., Alix, S., Henley, A., Di-Stefano, F., Ahmad, Z., Guillard, S. et al. (2007) Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Cancer Res. 67, 5840–5850
|
|
|
|
| phosphatidylinositol 4,5-bisphosphate
|
|
|
|
| peptidylprolyl isomerase–parvulin inhibitor PiB (diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn][3,8]phe- nanthroline-2,7-diacetate; Calbiochem) 17906639(C)
|
|
|
|
| Syk Inhibitor 12435267(D)
|
|
|
|
| a 24 amino acid fragment of PIF that encompasses the hydrophobic motif of PRK2 bound to a hydrophobic pocket on the small lobe of the kinase domain of PDK1, which was termed the PIF-binding pocket (Biondi et al., 2000). 11500365(C)
|
|
|
|
| Biondi,R.M., Cheung,P.C., Casamayor,A., Deak,M., Currie,R.A. and Alessi,D.R. (2000) Identi®cation of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA. EMBO J., 19, 979±988.
|
|
|
|
| cell-permeable myristoylated PKCz pseudosubstrate (Biosource International) 19414597(C)
|
|
|
|
| PKA inhibitor 12150925(C) from Calbiochem
|
|
|
|
| activates PKC 11283245(C)
|
|
|
|
| phorbal 12-myristate,13-acetate
|
|
|
|
| polyadenylic acid, a synthetic RNA analog
|
|
|
|
| a synthetic dsRNA analog made of polyadenylic-polyuridylic acid
|
|
|
|
| a synthetic ssRNA analog made of polycytidylic acid
|
|
|
|
| synthetic dsDNA 16713980(C) unclear as to whether it means:
|
|
|
|
| Double-stranded polymer containing a 2-base repeating unit Poly(dA-dT):Poly(dA-dT)
|
|
|
|
| Double-stranded polymer containing complementary strands Poly(dA):Poly(dT)
|
|
|
|
| a synthetic DNA which may take on a B-form conformation 17618271(C)
|
|
|
|
| 9. Ishii, K. J. et al. A Toll-like receptor-independent antiviral response induced by
double-stranded B-form DNA. Nature Immunol. 7, 40–48 (2006).
|
|
|
|
| polydeoxyinosinic-polydeoxycytidylic acid
|
|
|
|
| synthetic dsDNA 16713980(C) unclear as to whether it means:
|
|
|
|
| Double-stranded polymer containing a 2-base repeating unit Poly(dI-dC):Poly(dI-dC)
|
|
|
|
| Double-stranded polymer containing complementary strands Poly(dI):Poly(dC)
|
|
|
|
| polyguanylic acid, a synthetic RNA analog
|
|
|
|
| polyinosinic acid, a synthetic RNA analog
|
|
|
|
| a synthetic dsRNA analog polyinosinic-polycytidylic acid which is a ligand for TLR3 11607032(D)
|
|
|
|
| an antibiotic that binds to Lipid-A in LPS and blocks "biological effects" 17658277(C)
|
|
|
|
| Duff, G.W., and Atkins, E. (1982). The inhibitory effect of polymyxin B
on endotoxin-induced endogenous pyrogen production. J. Immunol.
Methods 52, 333–340.
|
|
|
|
| Palsson-McDermott, E.M., and O’Neill, L.A. (2004). Signal transduc-
tion by the lipopolysaccharide receptor, Toll-like receptor-4. Immunol-
ogy 113, 153–162.
|
|
|
|
| polyuridylic acid, a synthetic ssRNA analog.
|
|
|
|
| ligand for TLR7 and TLR8 15800576(C)->14976261,14976262
|
|
|
|
| Cr2O72−(aq) + 14H+ + 6e− → 2Cr3+(aq) + 7H2O (E = +1.33 V)
|
|
|
|
| 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo(3,4-d)pyrimidine
|
|
|
|
| 10202139(C): a specific inhibitor of Src family kinases (Daub et al., 1997)
|
|
|
|
| Daub,H., Wallasch,C., Lankenau,A., Herrlich,A. and Ullrich,A. (1997)
Signal characteristics of G protein-transactivated EGF receptor.
EMBO J., 16, 7032–7044.
|
|
|
|
| a specific inhibitor of Src kinases 16806820(C)
|
|
|
|
| 4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
|
|
|
|
| a negative control for PP1 and PP2
|
|
|
|
| 4-amino-7-phenylpyrazolo[3,4-d]pyrimidine
|
|
|
|
| a distinct ATP-compet- itive inhibitor of mTOR (Feldman et al., 2009) 19446321(C)
|
|
|
|
| Feldman, M.E., Apsel, B., Uotila, A., Loewith, R., Knight, Z.A., Ruggero, D., and Shokat, K.M. (2009). Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 7, e38.
|
|
|
|
| reduces cAMP "efflux" 16581779(C)
|
|
|
|
| Inhibits Ikkb 12556537(D) 15778223(C)
|
|
|
|
| Z-Ile-Glu(OtBu)-Ala-Leu-CHO
|
|
|
|
| Calbiochem 539160 Proteasome Inhibitor I
|
|
|
|
| A cell-permeable, reversible inhibitor of the chymotrypsin-like activity of the multicatalytic proteinase complex (MCP; 20S proteasome) in HT4 cells. Causes the accumulation of ubiquitinated proteins in neuronal cells. Prevents the activation of NF-κB in response to TNF-α and Okadaic Acid through inhibition of IκB-α degradation.
|
|
|
|
| Catalyzes ADP-Ribosylation of guanine nucleotide-binding regulatory proteins Gi, Go, Gt [Calbiochem]
|
|
|
|
| a specific inhibitor of Gnao/Gnai 16303557(C)
|
|
|
|
| Signals transduced from Gai proteins are inhibited by PTX, which ADP-ribosylates Gai proteins at their C terminus to prevent heir interaction with GPCRs. However, a flurry of recent studies suggest that although PTX induces ADP-ribosylation of Gai proteins and uncouples them from GPCRs, it does not impede the activation of Gai proteins by various accessory proteins, nor does it prevent the interaction of Gai proteins with their initiator or effector proteins (39). 19401591(C)
|
|
|
|
| 39. M. Sato, J. B. Blumer, V. Simon, S. M. Lanier, Accessory proteins for G proteins: Partners in signaling. Annu. Rev. Pharmacol. Toxicol. 46, 151–187 (2006).
|
|
|
|
| 1-hydroxypyridine-2-thione
|
|
|
|
| PyrrolidineDithiocarbamate
|
|
|
|
| a chemical inhibitor of Nfkb 17334236(C)
|
|
|
|
| PyrrolidineDithiocarbonate
|
|
|
|
| a metal chelator 8108390(C)
|
|
|
|
| an antiviral compound 17599095(C)
|
|
|
|
| an antiviral compound 17599095(C)
|
|
|
|
| CID: 159603 synonyms: Resiquimod S28463
|
|
|
|
| believed to mimic bacteria RNA [17785828(C)]
|
|
|
|
| a ligand for TLR7 and TLR8 [16895974]
|
|
|
|
| a known inducer of TLR7 17337443(C)
|
|
|
|
| Inhibits mTOR 11147790(D)
|
|
|
|
| The mode of action of Rapamycin is to bind the FKBP12. The Rapamycin-FKBP12 complex inhibits the mTOR pathway by directly binding the mTOR Complex1 (mTORC1). Rapamycin must bind FKBP12 first, and only the FKBP12-rapamycin complex can bind FRAP/RAFT/mTOR.
|
|
|
|
| 3,4′,5-Trihydroxy-trans-stilbene, 5-[(1E)-2-(4-Hydroxyphenyl)ethenyl]-1,3-benzenediol
|
|
|
|
| Resveratrol is a phenolic phytoalexin found in grape skin and other plants. It has intracellular antioxidant activity and activates SIRT1, a NAD+-dependent histone deacetylase involved in mitochondrial biogenesis and the enhancement of peroxisome proliferator-γ-activated receptor coactivator-1α (PGC-1α) and FOXO activity. The anti-diabetic, neuroprotective and anti-adipogenic actions of resveratrol may be mediated via SIRT1 activation. [Sigma catalog]
|
|
|
|
| an inhibitor of RNA-dependent RNA polymerase transcription 15367631(C)
|
|
|
|
| 35. Patterson, J. L., and R. Fernandez-Larsson. 1990. Molecular mechanisms of
action of ribavirin. Rev. Infect. Dis. 12:1139–1146.
|
|
|
|
| a synthetic ssRNA from HIV-1 U5 region nt 108-127 14976262(C)
|
|
|
|
| 5' GCCCGUCUGUUGUGUGACUC 3'
|
|
|
|
| 5" GsCsCsCsGsUsCsUsGsUsUsGsUsGsUsGsAsCsUsC 3'
|
|
|
|
| phosphothioate protected positions are indicated by ‘s’
|
|
|
|
| Dotap was complexed with the RNA to facilitate uptake
|
|
|
|
| a derivative of RNA40 in which all U's were reaplaced by A's 14976262(D)
|
|
|
|
| 5' GCCCGACAGAAGAGAGACAC 3'
|
|
|
|
| GsCsCsCsGsAsCsAsGsAsAsGsAsGsAsGsAsCsAsC
|
|
|
|
| phosphothioate protected positions are indicated by ‘s’
|
|
|
|
| Dotap was complexed with the RNA to facilitate uptake
|
|
|
|
| a derivative of RNA40 in which all G's were reaplaced by A's 14976262(D)
|
|
|
|
| 5' ACCCAUCUAUUAUAUAACUC 3'
|
|
|
|
| AsCsCsCsAsUsCsUsAsUsUsAsUsAsUsAsAsCsUsC
|
|
|
|
| phosphothioate protected positions are indicated by ‘s’
|
|
|
|
| Dotap was complexed with the RNA to facilitate uptake
|
|
|
|
| actually named: RNA9.2s 17038590
|
|
|
|
| synthetic RNA92s: 5’-OHAGCUUAACCUGUCCUUCAA-3'
|
|
|
|
| IVT RNA92s: 5’-pppAGCUUAACCUGUCCUUCAA-3'
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| Inhibits PKCs 11147790(D)(36)
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| inhibitor of cyclin-dependent kinases 16687404(C)
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| Meijer, L., Borgne, A., Mulner, O., Chong, J. P., Blow, J. J., Inagaki, N., Inagaki, M., Delcros, J. G., and Moulinoux, J. P. (1997) Eur. J. Biochem. 243, 527–536
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| CDK2-specific inhibitor (ID50 = 700 nM, specific for CDK1 and CDK2) (61, 62). 11359766(C)
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| 61. Rudolph, B., Saffrich, R., Zwicker, J., Henglein, B., Muller, R., Ansorge, W.,
and Eilers, M. (1996) EMBO J.
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| 15, 3065–3076 62. Meijer, L., Borgne, A., Mulner, O., Chong, J. P., Blow, J. J., Inagaki, N.,
Inagaki, M., Delcros, J. G., and Moulinoux, J. P. (1997) Eur. J. Biochem.
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| PPARg agonist 16143103(C) 14525654(C)
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| Rotenone works by interfering with the electron transport chain in mitochondria. To be specific, it inhibits the transfer of electrons from iron-sulfur centers in complex I to ubiquinone. This interferes with NADH during the creation of usable cellular energy (ATP).
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| PKC inhibitor 14651849(C)
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| PKCd inhibitor 1134345(C)
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| Stat3 inhibitor 21573184(C)
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| Salicylihalamide A was first isolated in 1997 by NCI scientists from an unidentified species of the marine sponge Haliclona. Through the NCI 60-cell antitumor screen, it was found that this N-acyl-enamine appended macrolactone exhibited similar activity to the bafilomycins, which are vacuolar proton ATPase (V-ATPase) inhibitors. V-ATPases are located on membranes of vacuoles, lysosomes, and other organelles, as well as on certain specialized plasma membrane. These proton pumps are responsible for the pH regulation of intracellular compartments of eukaryotes, which is essential for many cellular processes. Irregular V-ATPase activity is thought to contribute to the development of a variety of diseases such as cancer and osteoporosis, making V-ATPase a potential target for the development of pharmacological agents.
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| inhibitor of the v-ATPase that does not have other known targets (11–14). 22053050(C)
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| 11. M. Forgac, Nat. Rev. Mol. Cell Biol. 8, 917 (2007).
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| 12. B. J. Bowman, M. E. McCall, R. Baertsch, E. J. Bowman,
J. Biol. Chem. 281, 31885 (2006).
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| 13. M. R. Boyd et al., J. Pharmacol. Exp. Ther. 297, 114
(2001).
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| 14. M. Huss et al., J. Biol. Chem. 277, 40544 (2002).
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| a potent IL-6 superantagonist that competes with IL-6 for binding to surface IL-6 receptors and prevents the gp130 subunits from oligomerizing and initiating downstream signaling (Sporeno et al., 1996).
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| Sporeno, E., Savino, R., Ciapponi, L., Paonessa, G., Cabibbo, A., Lahm, A., Pulkki, K., Sun, R.X., Toniatti, C., Klein, B., and Ciliberto, G. (1996). Human interleukin-6 receptor super-antagonists with high potency and wide spectrum on multiple myeloma cells. Blood 87, 4510–4519.
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| P38 inhibitor 14699082(C) 9069290[7]
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| 11154262(C) P38g,P38d are insensitive to SB203580
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| inhibits TgfbR1 15280432(C) 12191474(C) 19556242(C) 18758450(C)
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| Inman, G. J., Nicols, F. J., Callahan, J. F., Harling, J. D., Gaster, L. M., Reith, A. D., Laping, N. J. and Hill, C. S. (2002a). SB-431542 is a potent and specific inhibitor of transforming growth factor-βsuperfamily type I activin receptor-like kinase receptors, ALK4, ALK5 and ALK7. Mol. Pharmacol. 62, 65-72.
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| Laping, N. J., Grygielko, E., Mathur, A., Butter, S., Bomberger, J., Tweed, C., Fornwald, J., Lehr, R., Harling, J. D., Gaster, L. M. et al. (2002). Inhibition of transforming growth factor (TGF)-β1-induced extracellular matrix with a novel inhibitor of the TGF-βtype I receptor kinase activity. Mol. Pharmacol. 62, 58-64.
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| Ikk2 inhibitor 16371247(C)
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| [41] A.B. Gomez, C. Mackenzie, A. Paul, R. Plevin, Br. J. Pharmacol. 146 (2005) 217.
[42] Y. Peng, M.R. Power, B. Li, T.J. Lin, J. Leukoc. Biol. 77 (2005) 975.
[43] H. Buss, A. Dorrie, M.L. Schmitz, E. Hoffmann, K. Resch, M. Kracht, J. Biol. Chem. 279 (2004) 55633.
[44] S.J. Jeong, C.A. Pise-Masison, M.F. Radonovich, H.U. Park, J.N. Brady, J. Biol. Chem. 280 (2005) 10326.
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| A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.
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| MKK6 inhibitor 11278290(C)
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| inhibits p38 MAP kinase; structure in first source
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| 6-(4-fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo(2,1-b)thiazole
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| Previously, our laboratory demonstrated the feasibility of such an approach by preparing a small-molecule mimetic of Smac and showed that it permeates cells readily and acts in a similar fashion as natural Smac in the cell while bypassing mitochondrial regulation (Li et al., 2004). The small-molecule mimetic is a synthetic, two-headed structure designed to resemble the N-terminal amino acid residues (AVPI) of Smac protein that interact with BIR domains of XIAP (Wu et al., 2000). 17996648(C)
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| Li, L., Thomas, R.M., Suzuki, H., De Brabander, J.K., Wang, X., and Harran, P.G. (2004). A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death. Science 305, 1471–1474.
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| Wu, G., Chai, J., Suber, T.L., Wu, J.W., Du, C., Wang, X., and Shi, Y. (2000). Structural basis of IAP recognition by Smac/DIABLO. Nature 408, 1008–1012.
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| Nfkb1 Inhibitor 16622218(C)
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| a cell-permeable peptide that binds to uncomplexed NFkB and prevents nuclear translocation of
NFkB (39).
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| 39. Lin, Y. Z., Yao, S. Y., Veach, R. A., Torgerson, T. R., and Hawiger, J. (1995)
J. Biol. Chem. 270, 14255–14258
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| BML-P600-0005 NF-κB SN50 cell permeable inhibitory peptide
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|
| Sequence contains the nuclear localization sequence (NLS residues 360-369) of the transcription factor NF-κB p50 linked to a peptide cell-permeablization sequence, the hydrophobic region (h-region) of the signal peptide of Kaposi fibroblast growth factor (K-FGF). Peptide inhibits translocation of the NF-κB active complex into the nucleus. In mouse endothelial LE-II cells induced with LPS, inhibition of NF-κB nuclear translocation was 88% at 50µg/ml (18 µM). In human monocytic THP-1 cells induced by LPS or TNFα there was 85% inhibition at 100µg/ml.
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| Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro
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| BML-P601-0500 NF-κB SN50M cell permeable control peptide
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| Inactive control peptide for the cell-permeable NF-κB inhibitory peptide SN50. Contains the nuclear localization sequence (NLS residues 360-369) of the transcription factor NF-κB p50 linked to the hydrophobic region (h-region) of the signal peptide of Kaposi fibroblast growth factor (K-FGF), except this control peptide has Lys363 to Asn and Arg364 to Gly. In mouse endothelial LE-II cells induced with LPS, SN50M peptide had no measureable effect on NF-κB translocation at 50 µg/ml.
In human monocytic THP-1 cells induced by LPS or TNFα, there was slight inhibition of nuclear transport at 100 µg/ml.
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| H-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Asn-Gly-Gln-Lys-Leu-Met-Pro-OH
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| activates soluble guanylate cyclase
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| (+)-S-Nitroso-N-acetylpenicillamine
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| S-nitroso-L-cysteine-ethyl-ester 16423564(M)
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| nitric oxide donor 16423564(C)
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| slow release NO donor 17018880(C)
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| HDAC inhibitor 18324520(C)
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|
| A four carbon acid, CH3CH2CH2COOH, with an unpleasant odor that occurs in butter and animal fat as the glycerol ester
|
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| short-chain fatty acid sodium butyrate (NaBT; ref. 6), a histone deacetylase inhibitor produced in the colon by breakdown of dietary fiber (7).
|
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| 6. Wang Q, Wang X, Hernandez A, Kim S, Evers BM. Inhibition of the phosphatidylinositol 3-kinase pathway contributes to HT29 and Caco-2 intestinal cell differentiation. Gastroenterology 2001;120:1381–92.
7. Hague A, Manning AM, Hanlon KA, Huschtscha LI, Hart D, Paraskeva C. Sodium butyrate induces apoptosis in human colonic tumour cell lines in a p53-independent pathway : implications for the possible role of dietary fibre in the prevention of large-bowel cancer. Int
J Cancer 1993;55:498–505.
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|
| Butyric acid has been associated with the ability to inhibit the function of histone deacetylase enzymes, thereby favoring an acetylated state of histones in the cell. Acetylated histones have a lower affinity for DNA than non-acetylated histones, due to the neutralisation of electrostatic charge interactions. In general, it is thought that transcription factors will be unable to access regions where histones are tightly associated with DNA (i.e. non-acetylated, e.g., heterochromatin). Therefore, it is thought that butyric acid enhances the transcriptional activity at promoters, which are typically silenced/downregulated due to histone deacetylase activity.
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| Braf inhibitor 19274086(C)
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|
| aka BAY 43-9006, Nexavar, Sorafenib tosylate
|
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|
| 2-Pyridinecarboxamide, 4-(4-((((4-chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl- 4-(4-(3-(4-chloro-3-trifluoromethylphenyl)ureido)phenoxy)pyridine-2-carboxyllic acid methyamide-4-methylbenzenesulfonate
|
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|
|
| Jnk inhibitor 16687404(C) 15069087(C) 15326485 12738796(C)
|
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|
| Calbiochem Cat#420119 Jnk Inhibitor II
|
|
|
|
| A potent, cell-permeable, selective, and reversible inhibitor of c-Jun N-terminal kinase (JNK) (IC50 = 40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3). The inhibition is competitive with respect to ATP. Exhibits over 300-fold greater selectivity for JNK as compared to ERK1 and p38-2 MAP kinases. Inhibits the phosphorylation of c-Jun and blocks cellular expression of IL-2, IFN-γ, TNF-α, and COX-2. Blocks IL-1-induced accumulation of phospho-Jun and induction of c-Jun transcription. A 50 mM (5 mg/454 µl) solution of JNK Inhibitor II (Cat. No. 420128) in DMSO is also available.
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|
| Stat3 SH2 domain peptide inhibitor (SPI), FISKERERAILSTKPPGTFLLRFSESSK 21573184(C)
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|
|
| a cAMP analog 10913189(C)
|
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|
|
| Sp-adenosine 3,5-cyclic monophothioate triethylamine salt
|
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|
|
| adenylate cyclase inhibitor 11042184
|
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|
|
| An indolocarbazole that is a potent PROTEIN KINASE C inhibitor which enhances cAMP-mediated responses in human neuroblastoma cells. (Biochem Biophys Res Commun 1995;214(3):1114-20)
|
|
|
|
| general kinase inhibitor??
|
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|
|
| Pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent, cell-permeable, and broad spectrum inhibitor of protein kinases. Inhibits protein kinase A (IC50 = 7 nM), CaM kinase (IC50 = 20 nM), myosin light chain kinase (IC50 = 1.3 M), Protein kinase C (IC50 = 700 pM), and protein kinase G (IC50 = 8.5 nM). Also inhibits platelet aggregation induced by collagen or ADP but has no effect on thrombin-induced platelet aggregation. Induces apoptosis in human malignant glioma cell lines. Arrests normal cells at the G1 checkpoint. Purity: ≥97% by HPLC. CAS 62996-74-1.
Ref.: Couldwell, W.T., et al. 1994. FEBS Lett. 345, 43. Nishimura, H. and Simpson, I.A. 1994. Biochem. J. 302, 271. Bruno, S., et al. 1992. Cancer Res. 52, 470. Kiss, Z. and Deli, E. 1992. Biochem. J. 288, 853. Vitale, M.L., et al. 1992. Neuroscience 51, 463. Hoffman, R. and Newland, E.S. 1991. Cancer Chemother. Pharmacol. 28, 102. Oka, S., et al. 1986. Agric. Biol. Chem. 50, 2723.
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|
| a PKC inhibitor 19561403(C)
|
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| Abl1 inhibitor 16182283(C)
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| CamkkS inhibitor 16497986(C)
|
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|
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| inhibits Camkk2 17459875(C)
|
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|
|
| inhibits CamKKs [11867640, 12540834] 17519230(C)
|
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|
| 1,8-Naphthoylene benzimidazole-3-carboxylic acid
|
|
|
|
| Src kinase inhibitor [11074000] 12810717(C) 14996911(C)
|
|
|
|
| SU6656 (an indolinone analog) is structurally not related to PP1 (a pyrazolo-pyrimidine) and does not inhibit the autophosphorylation of EGFR and PDGFR [31]. 16182283(C)
|
|
|
|
| [31] R.A. Blake, M.A. Broome, X. Liu, J. Wu, M. Gishizky, L. Sun, S.A. Courtneidge, SU6656, a selective Src family kinase inhibitor, used to probe growth factor signalling, Mol. Cell. Biol. 20 (2000) 9018 – 9027.
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|
| FgfR1 inhibitor 17724016(C)
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|
| a inhibitor of the Nfkb pathway 1971214(C) 12808024(C)
|
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|
|
| a polyanionic compound that inhibits and reverses the binding of NGF to its receptors 1850549(C)
|
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|
|
| Hosang, M. J Cell Biochem 29,265 (1985)
|
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|
|
| a selective and synthetic LXR agonist 14525954(C)
|
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|
| LxRa/b agonist 16143103(C)
|
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|
|
| an inhibitor of protein phosphatases 1 and 2A; isolated from Streptomyces spiroverticillatus
|
|
|
|
| aka 4,5,6,7-tetrabromobenzotriazole 4,5,6,7-Tetrabromo-2-azabenzimidazole
|
|
|
|
| tert-butylhydroquinone (tBHQ)
|
|
|
|
| tert-Butanol; 2-methyl-2-propanol
|
|
|
|
| Use in Alcohol trap assay for suppression of PA production 19114562(C)
|
|
|
|
| PLD preferentially utilizes primary alcohols over H2O in the transphosphatidylation reaction and generated a phosphatidylalcohol at the expense of PA. This occurs because the primary alcohol can position its hydrophobic tail in the membrane with its hydroxyl group adjacent to the phosphate group on the phospholipid, where the nucleophilic attack can take place with more efficiency than the hydrolysis reaction—in spite of the high concentration H2O. Tertiary alcohols such as tert-BtOH do not work because they do not insert themselves into the membrane in a manner that positions the hydroxyl group adjacent to the phosphate and there- fore can be used as negative controls.
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|
|
|
| trifluoperazine a Calmodulin antagonist 14709557(C)
|
|
|
|
| inhibits ER Ca2+-ATPase 17244528(C)
|
|
|
|
| inhibits the Ca2-ATPase pump to raise intracellular Ca2 11027280(C)
|
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|
|
| inhibits cytoplasmic calcium signaling by diverting Ca+2 released from the ER from the cytoplasm to outside of the cell (Westfall et al., 2003) 19561403(C)
|
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|
| Westfall TA, Hjertos B, Slusarski DC. Requirement for intracellular calcium modulation in zebrafish dorsal-ventral patterning. Dev Biol 2003;259:380-91
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|
|
| Thapsigargin is non-competitive inhibitor of a class of enzymes known by the acronym SERCA, which stands for sarco/endoplasmic reticulum Ca2+ ATPase.[1] Structurally, thapsigargin is classified as a sesquiterpene lactone, and is extracted from a plant, Thapsia garganica. It is a tumor promoter in mammalian cells. The anti-malarial drug artemisinin is also a sesquiterpene lactone, leading to a proposal that this class of drugs works by inhibiting the SERCA of malaria parasites such as Plasmodium falciparum[2][3]; this hypothesis awaits confirmation[4].
Thapsigargin raises cytosolic calcium concentration by blocking the ability of the cell to pump calcium into the sarcoplasmic and endoplasmic reticula which causes these stores to become depleted. Store-depletion can secondarily activate plasma membrane calcium channels, allowing an influx of calcium into the cytosol.
Thapsigargin is useful in experimentation examining the impacts of increasing cytosolic calcium concentrations. Wikipedia
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| The TIRAP peptide consisted of the antennapedia sequence (RQIKIWFQNRRMKWKK) positioned at the NH2-terminal end of mouse TIRAP aa 138–151.
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| NK-p-tosyl-L-lysine chloromethyl ketone
|
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|
|
| Inhibits trypsin-like serine proteinases. Irreversibly inactivates trypsin without affecting chymotrypsin. Prevents nitric oxide production by activated macrophages by interfering with transcription of the iNOS gene. Blocks cell-cell adhesion and binding of HIV-1 virus to the target cells. In macrophages, blocks nitric oxide synthase induced by interferon-g and lipopolysaccharides (EC50 = 80 µM). Prevents endonucleolysis accompanying apoptotic death of HL-60 leukemia cells and normal thymocytes. Purity: ≥95% by elemental analysis. RTECS XT5160000, CAS 4238-41-9.
Ref.: Griscavage, J.M., et al. 1995. Biochem. Biophys. Res. Commun. 215, 721. Kim, H., et al. 1995. J. Immunol. 154, 4741. Bourinbaiar, A.S. and Nagorny, R. 1994. Cell Immunol. 155, 230. Biro, A., et al. 1992. Eur. J. Immunol. 22, 2547. Bruno, S., et al. 1992. Leukemia 6, 1113. Lee, S.F. 1992. Infect. Immun. 60, 4032. Schmidt, H.H., et al. 1992. Mol. Pharmacol. 41, 615.
R: 36/37/38; S: 26-36
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| 3-(1’,4’dihydroxytetralyl)methylene-2-oxindo a tyrosine kinase inhibitor used in 83874483
|
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|
| synthesized as described: P. dalla Zonca, F. Buzzetti, S. Penco, A. Graziani, and P. M. Comoglio, submitted for publication
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| a PHD inhibitor 19762779(C)
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| 18. Nangaku M, Izuhara Y, Takizawa S, Yamashita T, Fujii-Kuriyama Y, Ohneda O, Yamamoto M, van Ypersele de Strihou C, Hirayama N, Miyata T. A novel class of prolyl hydroxylase inhibitors induces angio- genesis and exerts organ protection against ischemia. Arterioscler Thromb Vasc Biol. 2007;27:2548 –2554.
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|
| Topotecan (trade name Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor. It is a water-soluble derivative of camptothecin. [Wikipedia]
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|
|
| A potent mTOR kinase inhibitor 21464307(C)
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| 31. Thoreen CC, et al. (2009) An ATP-competitive mammalian target of rapamycin
inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem 284:
8023–8032.
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| Toxin B, Clostridium difficile
|
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|
|
| inhibts Rho, Rac, Cdc42 by glucosylation of a thronine residue (CalBio)
|
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| A glucosyltransferase that covalently links a glucose moiety on a critical threonine residue of Rho, Rac, and Cdc42 (38), thus impairing the docking of the GTPases on their effectors. 15060067(C)
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| N-tosyl-L-phenylalanine chloromethyl ketone
|
|
|
|
| White solid. Irreversible inhibitor of chymotrypsin. Useful for inhibiting chymotrypsin activity in trypsin preparations. Inhibits apoptosis in thymocytes. Blocks the induction of nitric oxide synthase by g-interferon and lipopolysaccharides (EC50 = 20 µM). Purity: ≥98% by TLC. RTECS XT5613500, CAS 402-71-1.
Ref.: Fearnhead, H.O., et al. 1995. FEBS Lett. 357, 242. Griscavage, J.M., et al. 1995. Biochem. Biophys. Res. Commun. 215, 721. Weaver, V.M., et al. 1993. Biochem. Cell Biol. 71, 488. Murakami, T., et al. 1991. Biochim. Biophys. Acta 1079, 279. Nierodzik, M.L., et al. 1991. J. Clin. Invest. 87, 229. Wilson, W.E., et al. 1989. J. Biol. Chem. 264, 17777.
R: 41; S: 26-36
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|
| N,N,N-tetrakis(2-pyridylmethyl)ethylenediamine
|
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|
|
| depletes zinc 14713952(C)
|
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|
|
| Pparg agonist 11009565(C)
|
|
|
|
| a specific inhibitor of multiple histone deactylases 11533489(D) (11) H. Kuo, C. D. Allis, Bioessays 20, 615 (1998).
|
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| HDAC inhibitor 18324520(C)
|
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|
|
| trichostatin A
Trichlostatin A
Tricostatin A
nchembio860-comp3
Antibiotic A-300
(R)-Trichostatin A
nchembio.147-comp4
nchembio.275-comp1
nchembio815-comp20
NCGC_TSA
nchembio852-compR31
1c3r
Trichostatin A (TSA)
SGCTO-002
T8552_SIGMA
NChemBio.2007.18-comp3
AIDS096139
C17H22N2O3
AIDS-096139
CID444732
LMPK01000055
Trichostatin A from Streptomyces sp.
A-300-I
NCGC00162453-01
NCGC00162453-02
NCGC00162453-03
LS-74195
A 300
TSA
|
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|
| Thyroid-stimulating hormone, thyrotropin
|
|
|
|
| Tunicamycin is mixture of homologous nucleoside antibiotics that inhibits the UDP-HexNAc: polyprenol-P HexNAc-1-P family of enzymes. In eukaryotes, this includes the enzyme GlcNAc phosphotransferase (GPT), which catalyzes the transfer of N-actelyglucosamine-1-phosphate from UDP-N-acetylglucosamine to dolichol phosphate in the first step of glycoprotein synthesis. Tunicamycin blocks the synthesis of all N-linked glycoproteins (N-glycans) and causes cell cycle arrest in G1 phase. It is used as an experimental tool in biology, e.g. to induce unfolded protein response[1]. Tunicamycin is produced by several bacteria, including Streptomyces clavuligerus and Streptomyces Iysosuperficus.
Wikipedia
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| Tyrphostin A1, Tyrophostin A1
|
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| partial agonist for OpRk1
|
|
|
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| an inhibitor of agonist-induced PLC activity [21] 9663394(C)
|
|
|
|
| 21. Thompson AK, Mostafapour SP, Denlinger LC, Bleasdale JE, Fisher
SK: The aminosteroid U-73122 inhibits muscarinic receptor
sequestration and phosphoinositide hydrolysis in SK-N-SH
neuroblastoma cells. A role for Gp in receptor compartmentation.
J Biol Chem1991, 266:23856-23862.
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|
| 12150925(C) mitochondrial uncoupler
|
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|
|
| Bernard, P.A., and Cockrell, R.S. (1979). The respiration of brain mitochondria and its regulation by monovalent cation transport. Biochim. Biophys. Acta 548, 173–186.
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| 18497260(C) mitochondrial proton gradient inhibitor
|
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|
|
| Mitochondrial metabolic inhibitor 17277771(C)
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|
|
| used when vanadate ion is not specified
|
|
|
|
| (Z)-3-[(2,4-Dimethyl-3-(ethoxycarbonyl)pyrrol-5-yl)methylidenyl]indolin-2-one
VEGF Receptor 2 Kinase Inhibitor I
|
|
|
|
| A highly selective, cell-permeable indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor (IC50 = 70 nM) for murine vascular endothelial growth factor receptor 2 (VEGF-R2; KDR/Flk-1). The inhibition is suggested to be competitive with respect to ATP. Does not inhibit PDGF, EGF, and IGF-1 RTK activities (IC50 > 100 µM).
|
|
|
|
| acts directly on the Ca2 channel to block Ca2[12615955(R)] 17287212(C)
|
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|
|
| blocks insulin release by inhibiting the influx of extracellular Ca2+ 17287212(C)
|
|
|
|
| microtubule-depolymerizing reagent that inhibits fusion between autophagosomes and lysosomes 111060023(C)->Hoyvik 1986
|
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|
|
| an antagonist specific to the LPA1 and LPA3 receptors 16199135(C)
|
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|
| a cell-permeable, selective inhibitor of IKK1/2 kinase activity (IC50 < 10 uM, Calbiochem). 17724016(C)
|
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|
| WGA blocks nuclear transport through the nuclear pore complex by binding to carbohydrate moieties on nucleoporins (27). 16595679(C)
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| 27. Finlay, D. R., and Forbes, D. J. (1990) Cell 60, 17–29
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| Inhibits Mlck IC50=200nM (Calbio)
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| Inhibits PI3K IC50=5nM (Calbio)
|
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|
| PpaRa agonist 12368907(C) 11009565(C) 14525954(C) 10542237(C)
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|
| Rock inhibitor 10436159 15536074 16760434(C)
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|
| Z-Asp-Glu-Val-Asp-fluoromethyl ketone
C110772
benzoylcarbonyl-aspartyl-glutamyl-valyl-aspartyl-fluoromethyl ketone
|
|
|
|
| Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH2F
|
|
|
|
| A potent, cell-permeable, and irreversible inhibitor of caspase-8 and granzyme B. Effectively inhibits influenza virus-induced apoptosis in HeLa cells. Also inhibits granzyme B. When using with purified native or recombinant enzyme, pretreatment with an esterase is required [CalBiochem].
|
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|
| Ref.: Takizawa, T., et al. 1999. Microbiol. Immunol. 43, 245. Martin, D.A., et al. 1998. J. Biol. Chem. 273, 4345. Sweeney, E.A., et al. 1998. FEBS Lett. 425, 61. Thornberry, N.A., and Lazebnik, Y. 1998. Science 281, 1312.
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| a Caspase-8 inhibitor 10692572(C)
|
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|
| an aldehyde proteasome inhibitor 8657102(C)
|
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|
| Benzyloxycarbonyl-Leu-Leu-phenylalaninal (Z-LLF-CHO) (49) was a generous gift of M. Orlowski and from Signal Pharmaceuticals. 8657102(M)
|
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| 49. Vinitsky, A., C. Michaud, J. C. Powers, and M. Orlowski. 1992. Inhibition of the chymotrypsin-like activity of the pituitary proteinase complex. Biochemistry 31:9421–9428.
|
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|
| slow-binding reversible inhibitor of chymotrypsin-like activity
|
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|
|
| Z-Llf-CHO
Z-Leu-leu-phe-al, ZLLF
Boc-leu-leu-phe-cho
CID5487496
N-Benzyloxycarbonyl-leucyl-leucyl-phenylalaninal
L-Leucinamide, N-((phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-2-phenylethyl)-
N-((Phenylmethoxy)carbonyl)-L-leucyl-N-(1-formyl-2-phenylethyl)-L-leucinamide
143839-79-6
|
|
|
|
| Zinc - used when actual compound is not reported
|
|
|
|
| Pi3k inhibitor 19953085(C)
|
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|
| 19953085 Yaguchi S, Fukui Y, Koshimizu I, Yoshimi H, Matsuno T, Gouda H, Hirono S, Yamazaki K, Yamori T (2006) Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor. J Natl Cancer Inst 98: 545–556
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|
|
| a mysterious pan-caspase inhibitor bought from Calbiochem (but not in their catalog) used in 12138192 under the name z-VAD
|
|
|
|
| possible PubChem CIDs: CID:5497171 CID:5716 CID:5497171 CID:5497170
|
|
|
|
| 16940186(C): a pan-caspase inhibitor
|
|
|
|
| 15607973(C): a pan-Caspase (apoptosis) inhibitor
|
|
|
|
| Z-Val-Ala-Asp-Fluoromethylketone
(Cat.# FK109)
An irreversible general caspase inhibitor, non-methylated form.PROTECT FROM MOISTURE. Useful for studies involving recombinant, isolated, and purified caspase enzymes. Unlike Z-VAD(OMe)-FMK (Cat. No. FK009), this inhibitor does not require pretreatment with esterase for in vitro studies.
Komoriya, A. et al., J. Exp. Med., 191:1819 (2000).
Weissner, C. et al., Cell. Mol. Biol., 46:53 (2000).
Misaghi, S., et al. 2004. Chem. Biol. 11, 1677.
|
|
|
|
| glucomannan polysaccharide purified from Saccharomyces cerevisiae
|
|
|
|
| benzyloxycarbonyltyrosyl-valyl-alanyl-aspartic acid fluoromethyl ketone
|
|
|
|
| synonyms: 1-butanol n-butanol Butyl alcohol n-butyl alcohol butanol 1-hydroxybutane Butan-1-ol Methylolpropane Propylcarbinol Propylmethanol
|
|
|
|
| As a primary alcohol, inhibits the production of PA via PC-PLD by competition with water during the PLD-dependent displacement of choline from PC, thus yielding phosphatidyl-butanol instead of PA.
|
|
|
|
| blocks cellular gucose utilization by indirectly inhibiting hexokinase 14651849(C)
|
|
|
|
| an imidazoquinoline compound, ligand for TLR7 and TLR8 16737960(C)
|
|
|
|
| an imidazoquinoline compound, ligand for TLR7 and TLR8 16737960(C)
|
|
|
|
| inhibits autophagic sequestration 11266458->Seglen 1982
|
|
|
|
| inhibits class III Pi3k 17244528(C)
|
|
|
|
| inhibits Pi3k 11060023->Blommaart 1997
|
|
|
|
| specific inhibitor of autophagosome formation 11060023->Seglen 1992
|
|
|
|
| 5′-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression. [Sigma catalog]
|
|
|
|
| Decitabine is an epigenetic modifier that inhibits DNA methyltransferase activity which results in DNA demethylation (hypomethylation) and gene activation by remodeling “opening” chromatin. Genes are synergistically reactivated when demethylation is combined with histone hyperacetylation. [Sigma catalog]
|
|
|
|
| Fluorouracil (5-FU or f5U) (sold under the brand names Adrucil, Carac, Efudex and Fluoroplex) is a drug that is a pyrimidine analog which is used in the treatment of cancer. It works through noncompetitive inhibition of thymidylate synthase. Due to its noncompetitive nature and effects on thymidine synthesis, 5-FU is frequently referred to as the "suicide inactivator". It belongs to the family of drugs called antimetabolites.
Wikipedia
|
|
|
|
| Adenosine kinase inhibitor 14978242(C)
|
|
|
|
| NSC 204984
5-Thio-D-glucose
a-D-Glucothiopyranose
5-Thio-a-D-glucopyranose
|
|
|
|
| The TAK1 inhibitor (5Z-7-oxo-zeaenol) was purchased from AnalytiCon Discovery GmbH (catalog number NP-009245).
|
|
|
|
| 43. Ninomiya-Tsuji, J., Kajino, T., Ono, K., Ohtomo, T., Matsumoto, M., Shiina, M., Mihara, M., Tsuchiya, M., and Matsumoto, K. (2003) J. Biol. Chem. 278, 18485–18490
|
|
|
|
| inhibits cAMP-specific phosphodiesterases IC50 = 25 uM
|
|
|
|
| inhibits cGMP-specific phosphodiesterases IC50=900 nM
|
|
|
|
| antagonist of AdoRa1 and AdoRa2a 9575299(C) 16497986(C)
|
|
|
|
| 8-(sulfophenyl) theophylline
|
|
|
|
| 1,25-dihydroxyvitamin D3 1,25(OH)2D3
|
|
|
|
| an IKK inhibitor 15199157(D)
|
|
|
|
| 30. Rossi, A., P. Kapahi, G. Natoli, T. Takahashi, Y. Chen, M. Karin, and M. G. Santoro. 2000. Anti-inflammatory cyclopentene prostaglandins are direct inhibitors of IkB kinase. Nature 403:103–108.
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|
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;){kind=small}
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;){kind=small}
;){kind=small}
;){kind=small}
;){kind=small}
;){kind=small}