Cayman CMPD101

CMPD101 is an inhibitor of g protein-coupled receptor kinase 2 (GRK2) and GRK3 (IC₅₀s = 18 and 5.4 nM, respectively).¹ It is selective for GRK2 and GRK3 over GRK1, GRK5, GRK6, and GRK7 (IC₅₀s = 3,100, 2,300, >30,000, and 25,000 nM, respectively), as well as Rho-associated kinase 2 (ROCK2) and PKCα (IC₅₀s = 1,400 and 8,100 nM, respectively). CMPD101 induces cAMP accumulation in HEK293 cells expressing human β₂-adrenergic receptors (EC₅₀ = 10 µM). In isolated human prostate strips, CMPD101 (50 µM) inhibits contractions induced by electrical field stimulation, norepinephrine, phenylephrine, endothelin-1 (Item No. 24127), and U-46619 (Item No. 16450).²

WARNING This product is not for human or veterinary use.