GRK6-IN-1

GRK6-IN-1 (Compound 18) is the inhibitor for G protein-coupled receptorkinase 6 (GRK6) with an IC50 of 3.8-8 nM. GRK6-IN-1 also inhibits GRK7, GRK5, GRK4 and GRK1 with IC50s of 6.4, 12, 22 and 52 nM, respectively. GRK6-IN-1 has the potential for the research of multiple myeloma[1].

Product Specifications

CAS Number

[2677786-61-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Aurora Kinase; G Protein-coupled Receptor Kinase (GRK) ; IGF-1R

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; GPCR/G Protein; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/grk6-in-1.html

Concentration

10mM

Purity

99.61

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

COC1=CC=CC2=NC(NCC3=CC=C(Cl)C=C3OC)=NC(NC4=NNC(CC)=C4)=C12

Molecular Formula

C22H23ClN6O2

Molecular Weight

438.91

Precautions

H315, H319, H320

References & Citations

[1]Uehling DE, et al. Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma [published correction appears in J Med Chem. 2022 Jan 13;65 (1) :886-887]. J Med Chem. 2021;64 (15) :11129-11147.|[2]George K, et al., Robust GRK2/3/6-dependent desensitization of oxytocin receptor in neurons. iScience. 2024 May 22;27 (6) :110047.