GRK2 Inhibitor 2

GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC50 of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC50 of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF) [1].

Product Specifications

CAS Number

[2592436-21-8]

UNSPSC

12352005

Target

Aurora Kinase; G Protein-coupled Receptor Kinase (GRK)

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/grk2-inhibitor-2.html

Purity

99.92

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C2=C(C=NN1CC3=CC(OC)=CC=C3)C=CC(C4=CNN=C4)=C2

Molecular Formula

C19H16N4O2

Molecular Weight

332.36

References & Citations

[1]Xu G, et al. Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg Med Chem Lett. 2020 Dec 1;30 (23) :127602.