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GPCR/G Protein GRK

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
T1636 Paroxetine hydrochloride Paroxetine hydrochloride is a serotonin uptake inhibitor that is effective in the treatment of depression.
T3498 CCG215022 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.
T3513 GSK180736A 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)...
T14989 CMPD101 CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1...
T13714L GRK2-IN-1 hydrochloride GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine. GRKs-IN-1 hydro...
T13714 GRK2-IN-1 GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine. GRKs-IN-1, Compound 14as, has...
Paroxetine hydrochloride
T1636CAS 78246-49-8
Paroxetine hydrochloride is a serotonin uptake inhibitor that is effective in the treatment of depression.
CCG215022
T3498CAS 1813527-81-9
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.
GSK180736A
T3513CAS 817194-38-0
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)...
CMPD101
T14989CAS 865608-11-3
CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1...
GRK2-IN-1 hydrochloride
T13714LCAS
GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine. GRKs-IN-1 hydro...
GRK2-IN-1
T13714CAS 2055990-90-2
GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine. GRKs-IN-1, Compound 14as, has...