CMPD101 (S3463-GRP)

CMPD101 is a potent, highly selective and membrane-permeable inhibitor of GRK2 and GRK3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50 of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.