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