| Gene Expression, Epigenetics, Nuclear Function | ||
|---|---|---|
| #2112 | Cycloheximide | Blocks protein biosynthesis by inhibiting protein elongation |
| #5927 | Doxorubicin | Inhibits DNA and RNA synthesis by intercalating the DNA helix; inhibits topoisomerase I |
| #2200 | Etoposide | Inhibits topoisomerase II resulting in DNA breakage; induces apoptosis |
| #9676 | Leptomycin B | Inhibits nuclear export activity of XPO1/exportin 1 |
| #9950 | Trichostatin A (TSA) | Inhibits class I and class II histone deactylases |
| Cell Growth and Death | ||
| RTKs | ||
| #4401 | Crizotinib | Inhibitor of ALK and ROS1 (ATP-competitive inhibitor) |
| #5083 | Erlotinib | Inhibits EGFR (ATP-competitive inhibitor) |
| #4765 | Gefitinib | Inhibits EGFR (active site inhibitor) |
| #9084 | Imatinib | Inhibits Bcr-Abl, PDGFR, c-Kit (active site inhibitor) |
| #12121 | Lapatinib | Inhibits EGFR and HER2 (ATP-competitive inhibitor) |
| #8705 | Sorafenib | Inhibits VEGFR and PDGFR; inhibits Raf kinases; induces autophagy |
| #12328 | Sunitinib | Broad RTK inhibitor (PDGFR, VEGFR, c-KIT, RET, CSF-1R, FLT-3/CD135) |
| #9842 | Tyrphostin AG 1478 | Inhibits EGFR |
| #12998 | Vatalanib | Broad RTK inhibitor (VEGFR, PDGFR-B, c-KIT) |
| MAP Kinase | ||
| #2222 | Anisomycin | Inhibits protein synthesis; activates stress-activated kinases (SAPK/JNK, p38-MAPK) |
| #11916 | Chelerythrine Chloride | Cell-permeable inhibitor of PKC; Activates SAPK/JNK and p38-MAPK; induces apoptosis in some cell lines |
| #12147 | PD184352 | Highly selective, noncompetitive inhibitor of MEK1 and MEK2 |
| #9900 | PD98059 | Highly selective inhibitor of MEK1 and MEK2; binds inactive forms and prevent activation by upstream kinases |
| #9903 | U0126 | Highly selective inhibitor of MEK1 and MEK2 |
| #8158 | SB202190 | Cell-permeable, highly specific inhibitor of p38-MAPK (ATP-competitive inhibitor) |
| #5633 | SB203580 | Cell-permeable inhibitor of p38-MAPK (inhibits PDK1 at higher concentrations) |
| #8705 | Sorafenib | Inhibits VEGFR and PDGFR; inhibits Raf kinases; induces autophagy |
| #8177 | SP600125 | Cell-permeable, highly specific inhibitor of JNK-family kinases |
| PI3 Kinase/Akt Pathway | ||
| #12017 | Everolimus | Specific inhibitor of mTORC1 protein complex |
| #9901 | LY294002 | Reversible but potent inhibitor of PI3K family members |
| #9904 | Rapamycin | Specific inhibitor of mTORC1 protein complex |
| #9951 | Wortmannin | Irreversible, potent inhibitor of PI3K faimly members |
| Other Kinases and Phosphatases | ||
| #9902 | Calyculin A | Cell permeable, selective inhibitor of PP1 and PP2A |
| #9052 | Dasatinib | Tyrosine kinase inhibitor (Abl, Bcr/Abl, Src, c-KIT, Ephrin receptors) |
| #9084 | Imatinib | Tyrosine kinase inhibitor (Abl, Bcr/Abl, c-KIT, PDGFR) |
| #12209 | Nilotinib | Tyrosine kinase inhibitor (Abl, Bcr/Abl, c-KIT, LCK, Ephrin receptors, DDR1/2, PDGFR-B) |
| #5934 | Okadaic Acid | Cell permeable, selective inhibitor of PP1, PP2A, and PP2B |
| #9493 | PKC412 | Very broad spectrum protein kinase inhibitor (conventional PKCs, some RTKs, Syk, Cdk1/B, c-Src, etc) |
| #9885 | Roscovitine | Potent and selective inhibitor of CDK1, 2, and 5 (ATP-competitive) |
| Cellular Metabolism | ||
| #9944 | AICAR | AMP analog that activates AMPK |
| #9996 | Oligomycin | ATP synthase inhibitor; inhibits oxidative phosphorylation |
| Calcium, cAMP, and Lipid Signaling | ||
| #9841 | Bisindolylmaleimide I, Hydrochloride | Potent inhibitor of PKC family members |
| #9973 | Cyclosporin A | Inhibits calcineurin |
| #9974 | FK-506 | Inhibits calcineurin |
| #3828 | Forskolin | Potent activator of adenylate cyclase, used to increase levels of cAMP |
| #12060 | Gö6976 | Potent inhibitor of calcium-dependent PKC family members |
| #9844 | H-89, Dihydrochloride | Broad spectrum Ser/Thr kinase inhibitor used to inhibit PKA; also inhibits the activity of p70S6K, MSK, and ROCKII and others |
| #9995 | Ionomycin, Calcium Salt | Calcium ionophore; activates calcium-/calmodulin-dependent kinase and calcium-dependent PKCs |
| #9953 | Staurosporine | Very broad, ATP-competitive protein kinase inhbitor (PKC, PKA, Src, CaM kinase, etc.) |
| #4174 | TPA (12-O-Tetradecanoylphorbol-13-Acetate) | Cell permeable, potent activator of PKC; also used to activate MAPK |
| Cell Biology | ||
| #8132 | 17-AAG | Inhibits HSP90 chaperone activity resulting in degradation of HSP90 client proteins |
| #2204 | Bortezomib | Proteasome inhibitor |
| #9972 | Brefeldin A | Inhibits ER to Golgi protein transport; triggers UPR and apoptosis |
| #9886 | Docetaxel | Inhibits microtubule depolymerization; prevents cell division |
| #9843 | Geldanamycin | Inhibits HSP90 chaperone activity resulting in degradation of HSP90 client proteins |
| #2194 | MG-132 | Proteasome inhibitor |
| #2190 | Nocodazole | Inhibits microtubule polymerization; induces cell cycle arrest in G2/M-phase |
| #9807 | Paclitaxel | Inhibits microtubule depolymerization; prevents cell division |
| #12758 | Thapsigargin | Inhibits ER calcium-ATPases; induces ER stress |
| #12819 | Tunicamycin | Inhibits glycoprotein synthesis and causes G1 cell cycle arrest |
Created September 2014
