产品
编 号:F755338
分子式:C26H24ClFN4O3
分子量:494.95
产品类型
结构图
CAS No: 2750414-35-6
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产品详情
生物活性:
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
体外研究:
Human GRKs (GRK1?GRK7) are classified into three subfamilies: GRK1 (GRK1 and GRK7), GRK2 (GRK2 and GRK3), and GRK4 (GRK4, GRK5, and GRK6).CCG273441 (compound 9j) shows moderate potency (GRK5 IC50=3.8 nM) but 1000-fold selectivity over GRK2 (IC50=4.8 μM).