GRK

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.

Cat. No.	Product name	CAS No.	Purity
T13714L	GRK2-IN-1 hydrochloride (2055990-90-2 free base)	T13714L	98%
T13714L	GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
T13714	CCG258208	2055990-90-2	98%
T13714	GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
T1636	Paroxetine hydrochloride	78246-49-8	99.91%
T1636	Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.
T8913	1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID	260555-42-8	99.78%
T8913	1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.
T14989	CMPD101	865608-11-3	99.01%
T14989	CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits ...
T27471	GSK299115A	864082-35-9	98.99%
T27471	GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.
T3513	GSK180736A	817194-38-0	98.16%
T3513	GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), b...
T27467	GSK270822A	864082-23-5	98.13%
T27467	GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.
T24850	Takeda103A	865609-72-9	98.01%
T24850	Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
T3498	CCG215022	1813527-81-9	97.46%
T3498	CCG215022 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.
T9609	GRK5-IN-2	1642839-27-7	98%
T9609	GRK5-IN-2, a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. It regulates the expression and/or release of in...
T61556	GRK6-IN-2	2677786-27-3	98%
T61556	GRK6-IN-2 is a potent G protein-coupled receptor kinase 6 (GRK6) inhibitor with potential antitumor activity.GRK6-IN-2 has been studied in multiple myeloma.