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Cat. No. Product Name CAS No. Information
PC-60585

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.

PC-45591

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.

PC-60588

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.
PC-60587

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.
PC-60586

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.
PC-60353

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.
PC-60352

GRK2-IN-115h

865608-11-3 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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