CCG-215022( CCG215022 | CCG 215022 )

Catalog No. M12785 CAS No. 1813527-81-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CCG-215022
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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.
In Vivo

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Synonyms

CCG215022 | CCG 215022
Pathway

Others
Target

GRK (GPCRK)
Recptor

GRK1|GRK2|GRK5|PKA
Research Area

Cancer
Indication

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CAS Number

1813527-81-9
Formula Weight

499.4964
Molecular Formula

C26H22FN7O3
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 28 mg/mL
SMILES

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
Chemical Name

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

1. Homan KT, et al. J Biol Chem. 2015 Aug 21;290(34):20649-59.

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