CCG-273220 是一种 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂，IC50为 220 nM。CCG-273220 能够与GRK5亚家族特异性残基 Cys474 共价结合，而对GRK5的选择性高于 GRK2。

CCG-273220 is a covalent inhibitor of G protein-coupled receptor ( GPCR ) kinase 5 ( GRK5 ) with an IC 50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC 50 =350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle [1].

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 IC 50 =220 nM) but 1500-fold selectivity over GRK2 (IC 50 =350 μM) [1].

2750414-35-6

C26H24ClFN4O3

494.95

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years