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.
Molekulargewicht:
542.57
CAS Nummer:
[3061801-11-1]
Formel:
C30H27FN4O5
Target-Kategorie:
GRK
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