GRK2-IN-1

Names

[ CAS No. ]:
2055990-90-2

[ Name ]:
GRK2-IN-1

Biological Activity

[Description]:

GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others

[Target]

GRK2:30 nM (IC50)

GRK5:7.1 μM (IC50)


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H25FN4O4

[ Molecular Weight ]:
452.48

Related Compounds