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Request The Product List ofGRK (GPCRK) GRK (GPCRK)

Cat. No. Product Name CAS No. Information
H9144

CCG273463

CCG273463 is a highly selective, potent, and covalent G protein-coupled receptor kinase 5 inhibitors with IC50 value of 9 nM.
H6079

Compound 101

 		865608-11-3

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101)?is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3; inhibits the desensitization of the G protein-activated inwardly-rectifying potassium current evoked by receptor-saturating concentrations of Met-Enk, DAMGO, endomorphin-2, and morphine in rat and mouse locus coeruleus neurons; produces complete inhibition of DAMGO-induced MOPr phosphorylation at Ser(375), arrestin translocation, and MOPr internalization in HEK 293 cells.
H6078

CCG-224406

 		1870843-22-3

A highly selective and potent GRK2 (G protein-coupled receptor kinase 2) inhibitor with IC50 of 130 nM; displays >700-fold selectivity over other GRK subfamilies, and no detectable inhibition of ROCK1.
H6077

CCG-215022

 		1813527-81-9

CCG-215022 (CCG215022) is a potent and selective pan GRK (G protein-coupled receptor kinase) inhibitor with IC50 of 0.15/0.38/3.9 uM for GRK2/5/1 respectively; displays 300-800 fold selectivity against PKA; exhibits improved potency compared with GSK180736A.
H6076

CCG 258748

A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM; displays 30-fold selectivity over GRK5, and no significant inhibitory activity against GRK1, PKA and ROCK1.
H6075

CCG 258001

 		2055990-96-8

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM; displays >100-fold selectivity over GRK5, GRK1, PKA and ROCK1.
H6074

CCG 224061

 		2055990-82-2

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 66 nM; displays >30-fold selectivity over GRK5, GRK1, PKA and ROCK1.
H6082

GSK-180736A

 		817194-38-0

A highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM; displays >400-fold selective for GRK2 over both GRK1 and GRK5, with no inhibition on PKA; also inhibits ROCK with IC50 of 0.1 uM.
H6081

GRK2-IN-115h hydrochloride

 		1941168-71-3

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM; showes enough selectivity against GRK1/5/6/7, ROCK2 and PKCα with equipotent inhibition to GRK3 (IC50=5.4 nM); potentiates βAR-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol; a novel potential agent for heart failure treatment.

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