CCG-215022

Research use only, not for human use.

CCG-215022 (CCG215022) is a potent and selective pan GRK inhibitor with IC50 of 0.15/0.38/3.9 uM for GRK2/5/1 respectively.

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.

CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2.

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CCG215022 | CCG 215022

Others

GRK (GPCRK)

GRK1|GRK2|GRK5|PKA

Cancer

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1813527-81-9

499.4964

C26H22FN7O3

>98% (HPLC)

DMSO: ≥ 28 mg/mL

O=C(C1=C(F)C=CC(C2C(C(NC3=CC=C(NN=C4)C4=C3)=O)=C(C)NC(N2)=O)=C1)NCC5=NC=CC=C5

4-(4-fluoro-3-((pyridin-2-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years