GRK5-IN-4

Names

[ CAS No. ]:
2410794-89-5

[ Name ]:
GRK5-IN-4

Biological Activity

[Description]:

GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

[Target]

IC50: 1.1 ± 0.4 μM (GRK5), 1.8 ± 2 μM (GRK6), >100 μM (GRK2)[1]


[In Vitro]

GRK5-IN-4 (Compound 16d) (0-4 h) displays a marked increase in apparent potency as a function of time[1].

[References]

[1]. Rowlands RA, et al. Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett. 2019 Nov 12;10(12):1628-1634.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H25N7O3

[ Molecular Weight ]:
483.52


Related Compounds

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