CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with anIC₅₀value of 3.8 nM. CCG273441 is highly selective toGRK5over GRK2 (IC₅₀=4.8 μM) by binding Cys474, aGRK5subfamily-specific residue, as a covalent handle^[1].

IC50: 3.8 nM (human GRK5), 19 nM (GRK5-C474S), 4.8 μM (bovine GRK2)^[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].
CCG273441 (compound 9j) shows moderate potency (GRK5 IC₅₀=3.8 nM) but 1000-fold selectivity over GRK2 (IC₅₀=4.8 μM)^[1].

494.95

Solid

C₂₆H₂₄ClFN₄O₃

2750414-35-6

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(101.02 mM;Need ultrasonic)

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