CMPD101

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure[1].

Product Specifications

CAS Number

[865608-11-3]

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

COVID-19-anti-virus

Field of Research

Cardiovascular Disease

Assay Protocol

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

Concentration

10mM

Purity

98.95

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F

Molecular Formula

C24H21F3N6O

Molecular Weight

466.46

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.|[2]Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.