PF-03622905

Modify Date: 2024-04-05 13:03:24

PF-03622905 Structure
PF-03622905 structure
Common Name PF-03622905
CAS Number 1072100-15-2 Molecular Weight 469.58
Density N/A Boiling Point N/A
Molecular Formula C24H35N7O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-03622905


PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases[1].

 Names

Name PF-03622905

 PF-03622905 Biological Activity

Description PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases[1].
Related Catalog
Target

PKCα:5.6 nM (IC50)

PKCβI:14.5 nM (IC50)

PKCβII:13 nM (IC50)

PKCγ:37.7 nM (IC50)

PKCθ:74.1 nM (IC50)

In Vitro PF-03622905 causes concentration-dependent inhibition of phospho-ERK1/2 formation, interleukin 8 release, and phospho-SHP2 levels with an IC50 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].
References

[1]. Stephan Grant, 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.

 Chemical & Physical Properties

Molecular Formula C24H35N7O3
Molecular Weight 469.58