2,3,4,5-Tetrahydro-7-hydroxy-1H-benzofuro[2,3-c]azepin-1-one

Acts as a potent and selective inhibitor of protein kinase D (PKD1) .

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, CaMKIIα, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 μM, including Akt1/2 and PKCα/β/δ/ζ. 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-3β, CKIδ, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 μM inhibitor = 95, 86, 82, 75, 71, and 50, respectively).

CID755673 is a cell-permeable, potent and selective inhibitor of all three protein kinase D (PKD) isoforms PKD1 (PKCμ), PKD2, and PKD3 (PKCν). CID755673 is not competitive with ATP.