|
PKD Inhibitor, CID755673
7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
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).
产品信息
Form Brown solid
Molar mass 217.2
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C12H11NO3
CAS number 521937-07-5
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |