PF-04577806 is a potent, selective, and ATP competitive inhibitor of the protein kinase C (PKC). It exhibits significant inhibitory activity against various isoforms of PKC, including PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, with IC50 values of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. Furthermore, PF-04577806 has the ability to reverse retinal vascular leakage in diabetic rats.

PKCε:522 nM (IC50), PKCβII:6.9 nM (IC50), PKCα:2.4 nM (IC50), PKCδ:586 nM (IC50), PKCθ:29.5 nM (IC50), PKCγ:45.9 nM (IC50), PKCβI:8.1 nM (IC50)

PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC 50 of 0.18 μM[1]. PF-04577806 (0.12-10 μM; pretreated for 60 min) inhibits phorbol myristate acetate-stimulated phosphorylation of ERK1/2 in Jurkat cells, with an IC 50 of 0.28 μM[1]. PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC 50 of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC 50 of 0.12 μM[1]. PF-04577806 (1 μM; 48 h) shows low cytotoxicity against human umbilical vein endothelial cells with remaining cell viability at 100.5% viable[1]. Western Blot Analysis[1]Cell Line: Jurkat T cells Concentration: 0, 0.12, 0.37, 1.11, 3.33, 10.0 μM Incubation Time: Pretreated for 1 hours Result: Showed a dose-dependent decrease in phospho-ERK1/2 but not total ERK1/2.