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].

Product Specifications

CAS Number

[1072100-81-2]

UNSPSC

12352005

Target

PKC; SHP2

Type

Reference compound

Related Pathways

Epigenetics; Protein Tyrosine Kinase/RTK; TGF-beta/Smad

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/pf-04577806.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C26H37N7O3

Molecular Weight

495.62

References & Citations

[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.