865608-11-3

865608-11-3 structure

Name: CMPD101
Chemical Name: 3-({[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide
CAS Number: 865608-11-3
Molecular Formula: C₂₄H₂₁F₃N₆O
Molecular Weight: 466.458
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2018-06-23 12:25:06
Modify Date: 2024-01-10 18:56:00
CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].

Name	3-({[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide
Synonyms	3-({[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide Benzamide, 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]- CMPD101

Description	CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Cardiovascular Disease Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> TGF-beta/Smad >> PKC Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK
Target	GRK2:18 nM (IC50) GRK3:5.4 nM (IC50) PKCα:8.1 μM (IC50) ROCK2:1.4 μM (IC50)
References	[1]. Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.