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CMPD101 (hydrochloride)

CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively) [1].

Product Specifications

CAS Number

1941168-71-3

UNSPSC

12352005

Target

G Protein-coupled Receptor Kinase (GRK) ; PKC; ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; GPCR/G Protein; Stem Cell/Wnt; TGF-beta/Smad

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/cmpd101-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F.[H]Cl

Molecular Formula

C24H22ClF3N6O

Molecular Weight

502.92

References & Citations

[1]Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60 (16) :6942-6990.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

GRK2; PKCα; ROCK2

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