CCG-273463

Names

[ CAS No. ]:
2750413-99-9

[ Name ]:
CCG-273463

Biological Activity

[Description]:

CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 9 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer[1].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Cardiovascular Disease

[Target]

IC50: 8.6 nM (GRK5), 12 μM (GRK2)[1].


[In Vitro]

CCG-273463 (0.02-1 μM) potently and highly inhibits GRK5 (IC50: 9 nM), with inhibitory rate of 93% (GRK5) and 97% (GRK6) at 1 μM[1].

[References]

[1]. Rachel A Rowlands, et al. Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem. 2021 Jan 14;64(1):566-585.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H25BrN4O3

[ Molecular Weight ]:
521.41

Related Compounds