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CCG273441

CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle[1].

Product Specifications

CAS Number

[2750414-35-6]

UNSPSC

12352005

Target

G Protein-coupled Receptor Kinase (GRK)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/ccg273441.html

Purity

98.78

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(/C(C1=C2)=C\C3=C(C(NC(CCl)=O)=C(N3)C)C)NC1=CC=C2C(N[C@@H](C4=CC=C(C=C4)F)C)=O

Molecular Formula

C26H24ClFN4O3

Molecular Weight

494.95

References & Citations

[1]Rowlands RA, et al. Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem. 2021 Jan 14;64 (1) :566-585.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

GRK2

Available Sizes

Curated Selection

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