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G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases within the AGC (protein kinase A, protein kinase G, protein kinase C) group of kinases. Like all AGC kinases, GRKs use ATP to add phosphate to serine and threonine residues in specific locations of target proteins. In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways.

GRK

货号 产品名 CAS号 信息
CSN22551 GSK180736A 817194-38-0 GSK180736A is an inhibitor of G protein-coupled receptor kinase 2 (GRK2) with IC50 of 0.77 μM.
CSN19161 CCG215022 1813527-81-9 CCG-215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.
CSN19106 AX20017 329221-38-7 AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.
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