PF-04577806 

PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC₅₀s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats^[1].

PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC₅₀ 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 IC₅₀ of 0.28 μM^[1].
PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC₅₀ of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC₅₀ 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

495.62

C₂₆H₃₇N₇O₃

1072100-81-2

O=C(C1=CC=CC=N1)NC2=NNC3=C2CN(C(N4[C@H](CN([C@@H](C4)C)CC5CCOCC5)C)=O)C3(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Grant S, et, al. Discovery of a novel class of targeted kinase inhibitors that blocks protein kinase C signaling and ameliorates retinal vascular leakage in a diabetic rat model. Eur J Pharmacol. 2010 Feb 10;627(1-3):16-25.  [Content Brief]