1072100-15-2

1072100-15-2 structure

Name: PF-03622905
Chemical Name: PF-03622905
CAS Number: 1072100-15-2
Molecular Formula: C₂₄H₃₅N₇O₃
Molecular Weight: 469.58
Catalog: Signaling Pathways Epigenetics PKC
Create Date: 2022-03-19 18:37:00
Modify Date: 2024-04-05 13:03:24
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].

Name	PF-03622905

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	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Metabolic Disease Signaling Pathways >> TGF-beta/Smad >> PKC
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.

Molecular Formula	C₂₄H₃₅N₇O₃
Molecular Weight	469.58