grk5

GRK5-IN-3 is a covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), significantly inhibiting GRK5 with an IC50 of 0.22 μM and GRK6 with an IC50 of 0.41 μM.

GRK5-IN-4 is a selective, potent, covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor (IC50: 1.1 μM).GRK5-IN-4 is 90 times more selective for GRK5 than GRK2.GRK5-IN-4 can be used to study heart failure.

GRK5-IN-2, a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. It regulates the expression and or release of insulin and is useful for the metabolic disease research.

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).

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.

GRL093-22 is an effective and selective inhibitor of G protein-coupled receptor kinases (GRK), with IC50 values of 60 nM for GRK5 and 40 nM for GRK6. It shows potential for research in heart failure and multiple myeloma.

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM for GRK2, 0.38±0.06 μM for GRK5, and 3.9±1 μM for GRK1.

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).

GRKs-IN-1 hydrochloride, Compound 14as, 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 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.

CCG-271423 is a potent and selective inhibitor of GRK5, demonstrating activity against GRK5 (IC50: 0.0021 μM) and GRK2 (IC50: 44 μM); it reduces Ca2+ transients and inhibits cardiomyocyte contractility.

CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) (IC50: 220 nM).CCG-273220 covalently binds the GRK5 subfamily-specific residue Cys474 and is more selective for GRK5 than GRK2.

CCG-273463 is a potent, covalent, selective inhibitor of GRK5 (IC50: 9 nM). CCG-273463 can be used to study heart failure, hypertrophic cardiomyopathy and cancer.

KR-39038 is an orally active GRK5 (G protein-coupled receptor kinase 5) inhibitor (IC50: 0.02 μM) that inhibits the HDAC5 pathway in neonatal cardiomyocytes and significantly reduces angiotensin II-induced hypertrophy, leading to notable anti-myocardial hypertrophy effects and improved cardiac function. KR-39038 is applicable for heart failure research.

GRL018-21 is a potent, highly selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 of 10 nM [1].

(S)-Ro 32-0432 is a potent, selective inhibitor of protein kinase C (PKC) and G protein-coupled receptor kinase 5 (GRK5), demonstrating ATP-competitive and oral activity. It presents IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε, showcasing its effectiveness against multiple PKC isoforms. Additionally, (S)-Ro 32-0432 inhibits T-cell activation, indicating its potential application in the research of chronic inflammatory and autoimmune diseases [1] [2].