GRK5-IN-5

GRK5-IN-5 (Compound 4a) is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5) with an IC50 value of 0.03 μM. It shows an IC50 of 2.2 μM for GRK2 and 0.036 μM for GRK6. GRK5-IN-5 exhibits potent anti-hypertrophic activity in cardiac muscle and inhibits the proliferation of non-cardiac cells. It blocks pathological cardiac remodeling by inhibiting the abnormal upregulation of hypertrophic marker genes Nppa and Nppb. GRK5-IN-5 is useful for research in myocardial hypertrophy.