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GRK2-IN-115h hydrochloride

GRK2-IN-115h hydrochloride Structure
GRK2-IN-115h hydrochloride structure
CAS No.
1941168-71-3
Chemical Name:
GRK2-IN-115h hydrochloride
Synonyms
CMPD101 hydrochloride;GRK2-IN-115h hydrochloride;GRK2 inhibitor 115h hydrochloride
CBNumber:
CB04844820
Molecular Formula:
C24H22ClF3N6O
Molecular Weight:
502.93
MDL Number:
MOL File:
1941168-71-3.mol
Last updated:2026-01-13 11:13:25
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GRK2-IN-115h hydrochloride Properties

storage temp. 2-8°C
solubility DMSO: 2mg/mL, clear
form powder
color white to beige
InChIKey QBLGBXYDINNUFE-UHFFFAOYSA-N
SMILES CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

WGK Germany  WGK 3
Storage Class 11 - Combustible Solids

GRK2-IN-115h hydrochloride price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML2784 CMPD101 hydrochloride ≥98% (HPLC) 1941168-71-3 5MG $144 2026-04-30 Buy
Sigma-Aldrich SML2784 CMPD101 hydrochloride ≥98% (HPLC) 1941168-71-3 25MG $577 2026-04-30 Buy
Biosynth RCD16871 Cmpd101 hydrochloride 1941168-71-3 25mg $813 2026-06-05 Buy
Biosynth RCD16871 Cmpd101 hydrochloride 1941168-71-3 50mg $1300.5 2026-06-05 Buy
Biosynth RCD16871 Cmpd101 hydrochloride 1941168-71-3 100mg $1809 2026-06-05 Buy
Product number Packaging Price Buy
SML2784 5MG $144 Buy
SML2784 25MG $577 Buy
RCD16871 25mg $813 Buy
RCD16871 50mg $1300.5 Buy
RCD16871 100mg $1809 Buy

GRK2-IN-115h hydrochloride Chemical Properties,Uses,Production

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-targeting, potent 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

GRK2-IN-115h hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

GRK2-IN-115h hydrochloride Suppliers

Global( 3)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 29874 58
Supplier Advantage
TargetMol Chemicals Inc. 58

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