GRK6-IN-1

GRK6-IN-1 (also known as Compound 18) is a potent, selective, small-molecule inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 3.8–8 nM. It also inhibits other GRK family members with lower potency, including GRK7 (IC50 of 6.4 nM), GRK5 (IC50 of 12 nM), GRK4 (IC50 of 22 nM), and GRK1 (IC50 of 52 nM). Developed by the Ontario Institute for Cancer Research (OICR) and the University Health Network (UHN), GRK6-IN-1 is primarily used as a research tool to study the role of GRK6 in multiple myeloma, hepatocellular carcinoma, and other biological processes such as PKD1 trafficking to primary cilia and oxytocin receptor desensitization.

Other names

GRK6 inhibitor 18GRK-6 inhibitor 18GRK 6 inhibitor 18N-(4-chloro-2-methoxybenzyl)-4-((5-ethyl-1,2-dihydro-3H-pyrazol-3-ylidene)amino)-5-methoxyquinazolin-2(1H)-imine