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
phosphodiesterase III inhibitor resulting in accumulation of cyclic AMP  14978242(C)
acetyltransferase inhibitor 17074756(C)
11069105(C) inhibitor of oxidative phosphorylation
12150925(C) an electron transport inhibitor
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.
To exclude the possible adenosine effect in nucleotide-induced AMPK activation, we inhibited 5'-nucleotidase 16497986(C)
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).
31. Spencer, D. M., Wandless, T. J., Schreiber, S. L., and Crabtree, G. R. (1993) Science 262, 1019 –1024
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
JNK/SAPK activator arsenite (45) 10232608(C)
38. Chen, C., and Okayama, H. High-efficiency transformation of mammalian cells by plasmid DNA. Mol. Cell. Biol., 7: 2745–2752, 1987.
Arsenic chloride 19276070(C)
RaR agonist 16143103(D)
a V-ATPase inhibitor
accumulates autophagosomes under starvation conditions 11060023(C)
Inhibits fusion between autophogosomes and lysosomes 11060023(C)->Hoyvik 1986
inhibitor of acidification of the endosomes 12900525(C)
[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
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)
32. Kuma, Y., Sabio, G., Bain, J., Shpiro, N., Marquez, R., and Cuenda, A. (2005) J. Biol. Chem. 280, 19472–19479
PubMed CID 16211152
stimulates TLR1/TLR2 15241416(C)
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.
Thiazolidenedione ligand for PPARg
transcriptional activation of acyl-CoA oxidase promoter construct
Pparg agonist 11009565(C)
Bovine Serum Albumin
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)
26 N-hexanoylsphingosine 9020886(C)
induces a slow increased in Ca2+ , autophagy, and autophagy-dependent cell death 17244528(C)
Kegg C01673 Calcitrol
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)
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.
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
DNA-damaging agent 16571722
DNA topoisomerase inhibitor (CalBio)
Induces apopotosis 16260609
PubChem CID 5831
A slowly hydrolyzed cholinergic agonist that acts at both muscarinic and nicotinic receptors
Pubchem CID 2554
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)
inhibits the mitogen-activated protein kinase-interacting kinase Mnk1 [Pubchem]
Src inhibitor 17646016(C)
AdoRa2a selective agonist 12082090(C)
used in 14747473
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)
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
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
used to dimerize proteins tagged with bacterial gyrase B (GyrB)
synthetic oligodeoxynucleotides of approx 8−30 bases in length that contain one or more CpG motifs of unmethylated CpG dinucleotides in certain base contexts
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
used in: 11812998
5'- ggTGCATCGATGCAgggggG -3'
used in: 15800576 16306936
negative control: gGTGCATCTATGCAGGGGgg
negative control: tcaagtgttctc
Cholera Toxin B-subunit
Wiki: binds to ganglioside GM1
used for visualizing GM1-gangliosides in lipid rafts 16880211(D)
used in 14716310 without explanation
kinase inhibitor 18456659(C)
beta-cyclodextrin is known to disrupt cholesterol-rich caveolae 18356165(C)
inhibits calcineurin 17519230(C)
inhibits PP2B 17079228(C)
Shortens actin filaments by blocking monomer addition at the fast-growing end of polymers
ROS in cells cause oxidation of DCFH, yielding the fluorescent product 2,7-dichlorofluorescein (DCF) 15265871(C)
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  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)
an inhibitor of JNK signaling 15142038(C)
a phosphodiesterase V/VI inhibitor 17292863(C)
contraction mimetic 17292863(C)
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)
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
PubChem CID 3165
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
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 .
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)
irreversible inhibitor of Rsk 17360704(D)
activates adenyl cyclases at 4 uM
increases cyclic-AMP levels
farnesyl transferase inhibitor 12842888(C)
a transfection reagent
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)
inhibitor of PKA PKG PKC from Calbiochem 12150925(C)
CamK2 30 uM
Casein Kinase 1 38 uM
MLK 28 uM
PKA 48 nM
Pkc 32 uM
Src inhibitor 11907028(C)
Humanized monoclonal antibody to ErbB2 gamma1-chain
human-mouse monoclonal rhuMab HER2 gamma1-chain, disulfide with human mouse monoclonal rhuMab
Trastuzumab, Trastuzumab [INN]
HER2 light chain, dimer
Immunoglobulin G1, anti-(human p185neu receptor
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
Inhibits cAMP and cGMP phosphodiesterases which causes increase in cAMP and PKA-act
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.
[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).
CID: 57469 aka R837
TLR7 ligand 16604075(C)
cyclooxygenase inhibitor 
a cyclooxygenase-1/cyclooxygenase-2 inhibitor 
a Ca2+ ionophore that serves as a mobile Ca2+ carrier that equilibrates Ca2+ levels across biological membranes, including plasma and ER membranes 17244528(C)
AdRb2 agonist 12082090(C)
Cramer, L. P. (1999). Role of actin-filament disassembly in lamellipodiumprotrusion in motile cells revealed using the drug jasplakinolide. Curr. Bio9, 1095-1105.
Inhinits actin disassemly?
a cell permeable peptide inhibitor from Calbiochem 12738796(C)
metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor
staurosporinone k-252a k-252b K252a 3'-(S)-epi-K-252a K 252a K 252b K 252c K 252d K-252c
Potassium Dichromate 19276070(C)
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.
22. Ando R, Hama H, Yamamoto-Hino M, Mizuno H, Miyawaki A (2002) Proc Natl Acad Sci USA 99:12651–12656.
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)
inhibitor of Gsk3
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
production of glutamate from alpha-ketoglutarate during transamination of leucine to alpha-ketoisocaproic acid  17287212(C)
blocks phagocytosis by stablizing actin 15711573(C)
Btk inhibitor 15849198(C) 16415872(C)
a synthetic RXR agonist 14525954(C)
Inhibits GSK3 11147790(D)
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]
a transfection reagent
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.
[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.
an inhibitor of Crml nuclear export pathway 16624523(C)
a specific inhibitor of NES-dependent intracellular transport 11265759(C)
refs cited - can't copy
a specfic inhibitor for Crm1 (Xpo1)
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.
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.
Lipoteichoic acid, Teichoic acid
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
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)
PubChem CID: 162771
disrupts cholesterol 12717440(C)
Simons,K.& Toomre,D.Lipid rafts and signal transduction.Nature Rev. Mol. Cell Biol. , 31–39 (2000).
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. 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.]
14713952(C): depletes cholesterol
a growth factor-independent energy source 17237771(C)
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)
26S Proteasome inhibitor 10587642(C)
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).
dimethyloxalylglycine - an ester of N-oxalylglycine that penetrates cells
an alkylating agent 12110590(C) 7737130(C)
an inducer of JnkS and P38S 12110590(C)
methyl methane sulfonate
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  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
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42. Peavy, D. E., Edmondson, J. W., and Duckworth, W. C. (1984) Endocrinology 114, 753–760
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)
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.
inhibitor of Slc29a1 16497986(C)
lipooxygenase inhibitor 
PubChem CID: 4362
A sulfhydryl reagent that is widely used in experimental biochemical studies.
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)
inhibitor of protein tyrosine phosphatases (PTPases) previously shown to be selective in preventing dephosphorylation of FAK and paxillin 10655584(D)33,34.
inhibitor of endocyctosis 12093727(C)
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).
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
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)  15304344(C)
 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.
Inhibits MEK 11147790(D)
activates PKC 11283245(C)
phorbol 12,13 dibutyrate
activates PKD 11784866(C)
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)
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.
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'
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'
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'
Inhibits PKCs 11147790(D)(36)
inhibitor of cyclin-dependent kinases 16687404(C)
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
PPARg agonist 16143103(C) 14525654(C)
PKC inhibitor 14651849(C)
P38 inhibitor 14699082(C) 9069290
11154262(C) P38g,P38d are insensitive to SB203580
inhibits TgfbR1 15280432(C) 12191474(C)
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.
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.
Ikk2 inhibitor 16371247(C)
 A.B. Gomez, C. Mackenzie, A. Paul, R. Plevin, Br. J. Pharmacol. 146 (2005) 217.  Y. Peng, M.R. Power, B. Li, T.J. Lin, J. Leukoc. Biol. 77 (2005) 975.  H. Buss, A. Dorrie, M.L. Schmitz, E. Hoffmann, K. Resch, M. Kracht, J. Biol. Chem. 279 (2004) 55633.  S.J. Jeong, C.A. Pise-Masison, M.F. Radonovich, H.U. Park, J.N. Brady, J. Biol. Chem. 280 (2005) 10326.
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.
MKK6 inhibitor 11278290(C)
Pubchem CID 5228
inhibits p38 MAP kinase; structure in first source
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)
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.
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.
Synonym: Compound 3
Nfkb1 Inhibitor 16622218(C)
a cell-permeable peptide that binds to uncomplexed NFkB and prevents nuclear translocation of NFkB (39).
39. Lin, Y. Z., Yao, S. Y., Veach, R. A., Torgerson, T. R., and Hawiger, J. (1995) J. Biol. Chem. 270, 14255–14258
activates soluble guanylate cyclase
nitric oxide donor 16423564(C)
slow release NO donor 17018880(C)
HDAC inhibitor 18324520(C)
A four carbon acid, CH3CH2CH2COOH, with an unpleasant odor that occurs in butter and animal fat as the glycerol ester
short-chain fatty acid sodium butyrate (NaBT; ref. 6), a histone deacetylase inhibitor produced in the colon by breakdown of dietary fiber (7).
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.
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.
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.
a cAMP analog 10913189(C)
Sp-adenosine 3,5-cyclic monophothioate triethylamine salt
adenylate cyclase inhibitor 11042184
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??
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.
SU6656 (an indolinone analog) is structurally not related to PP1 (a pyrazolo-pyrimidine) and does not inhibit the autophosphorylation of EGFR and PDGFR . 16182283(C)
 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.
a selective and synthetic LXR agonist 14525954(C)
LxRa/b agonist 16143103(C)
inhibits PP1 17079228(C)
inhibits ER Ca2+-ATPase 17244528(C)
inhibits the Ca2-ATPase pump to raise intracellular Ca2 11027280(C)