Activators & Inhibitors

Activity: Src kinase inhibitor . Function/Pharmacology: Src-I1 is a potent and competitive dual site (ATP- and peptide-binding) Src kinase inhibitor (IC50’s = 44 nM for Src and 88 nM for Lck). Also inhibits VEGFR2 (IC50 = 320 nM). Chemical Name: 6,7-Dimethoxy-N-(4-Phenoxyphenyl)-4-quinazolinamine

Activity: MAG lipase inhibitor . Function/Pharmacology: Inhibits MAG lipase (IC50=8 nM) selectively over FAAH. Irreversible. Cell permeable. Chemical Name: 4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxyl)methyl)piperidine-1-carboxylate

Activity: p38a MAP kinase inhibitor . Function/Pharmacology: JX401 is a potent, cell-permeable inhibitor of p38α (IC50 = 32 nM). No inhibition of p38β was observed at 10 µM. Chemical Name: 1-[2-Methoxy-4-(methylthio)benzoyl]-4-(phenylmethyl)piperidine

Activity: NGFR kinase inhibitor . Function/Pharmacology: GW-441756 is a potent and selective TrkA kinase inhibitor (IC50 = 2 nM). Chemical Name: 1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one

Activity: CHK2 inhibitor . Function/Pharmacology: Potent selective inhibitor of Chk2 (IC50 = 15 nM). BML-277 has been screened against a panel of 35 kinases, and shows less that 25% inhibition of any other kinase at 10 µM, demonstrating the selectivity1. Also displays radioprotective activity, preventing apoptosis in human T-cells that were subjected to ionizing radiation (EC50 = 3.0 – 7.6 µM). Chemical Name: 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide

Activity: CDK5/p25 inhibitor . Function/Pharmacology: Potent inhibitor of Cdk5/p25 (IC50 = 64 nM) and Cdk2 (IC50 = 98nM).1 Chemical Name: N-(5-isopropyl-thiazol-2-yl)phenylacetamide

Activity: PKC inhibitor . Function/Pharmacology: Potent and selective protein kinase C inhibitor (IC50 = 10 nM; cAMP-dependent protein kinase IC50 = 2 µM and phosphorylase kinase IC50 = 0.7 µM). Inactive against the tyrosine kinases EGFR, PGDFR and Insulin receptor. Potent inhibitor of GSK-3β in cell lysates (IC50 = 360nM) and GSK-3β immunoprecipitates (IC50 = 170nM) derived from rat epididymal adipocytes.2 Cell permeable. Chemical Name: 2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide

Activity: VEGFR / PDGFR kinase inhibitor . Function/Pharmacology: Potent selective inhibitor of VEGFR kinase (also known as Flk-1 and KDR). Inhibition of the activated kinase (IC50 = 0.4 µM) is 100-fold less than inhibition of the unactivated kinase (IC50 = 0.04 µM). Also inhibits PDGFR kinase (IC50 = 19.4 µM). Chemical Name: 3-(4-Dimethylaminobenzylidene)-1,3-dihydroindol-2-one

Activity: MMP-13 inhibitor . Function/Pharmacology: Selective inhibitor of MMP-13 (IC50 = 10 µM). It displayed no activity against MMP-1, MMP-9 or TACE. Chemical Name: N-[4-(4-Morpholinyl)butyl]-2-benzofurancarboxamide