GRK2-IN-115h hydrochloride

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM; showes enough selectivity against GRK1/5/6/7, ROCK2 and PKCα with equipotent inhibition to GRK3 (IC50=5.4 nM); potentiates βAR-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol; a novel potential agent for heart failure treatment.

References 1. Okawa T, et al. J Med Chem. 2017 Aug 24;60(16):6942-6990. View Related Products by Target GRK (GPCRK)