GRK5-IN-5

GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC₅₀ of 0.03 μM. GRK5-IN-5 shows IC₅₀ values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy.

• Data Sheet (267 KB)