grk2i

GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. Corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.

GRK2i TFA, a GRK2 inhibitory polypeptide, specifically targets and inhibits the activation of GRK2 by Gβγ. It mimics the Gβγ-binding domain, functioning as a cellular antagonist of Gβγ [1].

GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).

GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).

GRK2 Inhibitor is an effective GRK2 inhibitor. It enhances GPCR signaling by preventing receptor desensitization, used for heart failure and cardiovascular remodeling research.

CCG258208 hydrochloride (compound 14as hydrochloride) is a highly potent and selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 30 nM. It exhibits >200-fold selectivity for GRK2 over GRK5 (IC50 = 7.1μM). In cardiovascular research, CCG258208 effectively enhances the contractility of beta-AR-stimulated cardiomyocytes by inhibiting GRK2 activity. Additionally, the compound demonstrates excellent in vivo stability, making it a valuable tool for studying GRK2-related conditions such as heart failure.

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].