grk2 inhibitor 2

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293 cells. It is utilized in congestive heart failure (HF) research [1].

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2 3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

GRK2 Inhibitor is an inhibitor of β-Adrenergic Receptor Kinase 1 (β ARK1).

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

CMPD101 hydrochloride is a membrane-permeable small molecule inhibitor of GRK2 and GRK3, exhibiting IC50 values of 18 nM and 5.4 nM, respectively. This compound also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα, with IC50 values of 1.4 μM and 8.1 μM, respectively.