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Description

A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ, isoforms 1, 2, & 3 (IC50 = 182, 280, and 227 nM, respectively), while exhibiting >=30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIalpha, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µ,M, including Akt1/2 and PKCalpha/beta/delta/zeta. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser742 and Ser916 in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3beta, CKIdelta, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µ,M inhibitor = 95, 86, 82, 75, 71, and 50, respectively)., A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ, isoforms 1, 2, & 3 (IC50 = 182, 280, and 227 nM, respectively), while exhibiting >=30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIalpha, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µ,M, including Akt1/2 and PKCalpha/beta/delta/zeta. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser742 and Ser916 in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3beta, CKIdelta, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µ,M inhibitor = 95, 86, 82, 75, 71, and 50, respectively).