|Cat. No.||Product Name||CAS No.||Information|
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.
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.
CCG 258748 (CCG258748;CCG-258748) is 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.
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.
CCG 224061 (CCG224061;CCG-224061) is 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.
CCG 258001 (CCG258001;CCG-258001) is 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.
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