2750414-35-6

2750414-35-6 structure

Name: CCG-273220
Chemical Name: CCG-273220
CAS Number: 2750414-35-6
Molecular Formula: C₂₆H₂₄ClFN₄O₃
Molecular Weight: 494.95
Catalog: Research Areas Cancer
Create Date: 2022-11-13 18:32:23
Modify Date: 2024-04-05 19:46:21
CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC50=350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle[1].

Name	CCG-273220

Description	CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC50=350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle[1].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease
Target	IC50: 220 nM (GRK5)[1]
In Vitro	Human GRKs (GRK1−GRK7) are classified into three subfamilies: GRK1 (GRK1 and GRK7), GRK2 (GRK2 and GRK3), and GRK4 (GRK4, GRK5, and GRK6)[1]. CCG-273220 (compound 9e) shows moderate potency (GRK5 IC50=220 nM) but 1500-fold selectivity over GRK2 (IC50=350 μM)[1].
References	[1]. Rowlands RA, et al. Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem. 2021 Jan 14;64(1):566-585.

Molecular Formula	C₂₆H₂₄ClFN₄O₃
Molecular Weight	494.95