| Identification | Back Directory | [Name]
GRK2-IN-115h hydrochloride | [CAS]
1941168-71-3 | [Synonyms]
GRK2-IN-115h hydrochloride
GRK2 inhibitor 115h hydrochloride | [Molecular Formula]
C24H22ClF3N6O | [MOL File]
1941168-71-3.mol | [Molecular Weight]
502.93 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
CMPD101 is an active site-targetingpotent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2)but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo. | [IC 50]
PKCα: 8.1 μM (IC50); ROCK2: 1.4 μM (IC50) | [References]
[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. DOI:10.1021/acs.jmedchem.7b00443 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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