PF-03622905, a potent and ATP-competitive PKC inhibitor, exhibits IC50 values of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. Notably, PF-03622905 demonstrates high specificity for PKC in comparison to other protein kinases.

PKCβII:13 nM (IC50), PKCβI:14.5 nM (IC50), PKCγ:37.7 nM (IC50), PKCθ:74.1 nM (IC50), PKCα:5.6 nM (IC50)

PF-03622905 causes concentration-dependent inhibition of phospho-ERK1/2 formation, interleukin 8 release, and phospho-SHP2 levels with an IC 50 value 0.15 μM, 0.16 μM, and 35 nM, respectively[1]. PF-03622905 shows low cytotoxicity at 1 μM against human umbilical vein endothelial cells with remaining cell viability at 83.3% viable[1].