KR-39038

KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research[1].

Product Specifications

CAS Number

[2770300-35-9]

UNSPSC

12352005

Target

G Protein-coupled Receptor Kinase (GRK) ; HDAC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/kr-39038.html

Purity

99.68

Solubility

DMSO : 115 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

O=C1N=C(C2=C(Cl)C=CC=C2)NC3=CC(NCCCNCCCCNCCCN)=C(C=C13)F

Molecular Formula

C24H32ClFN6O

Molecular Weight

475.00

References & Citations

[1]Lee JH, et al. KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure. Biomol Ther (Seoul) . 2020 Sep 1;28 (5) :482-489.