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CCG-273220

  Cat. No.:  DC72121  
Chemical Structure
2750414-35-6
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More than 5000 active chemicals with high quality for research!
Field of application
CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC50=350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2750414-35-6
Chemical Name: CCG-273220
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
Formula: C26H24ClFN4O3
M.Wt: 494.95
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
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MSDS_36431_DC72121_2750414-35-6
COA
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Cat. No. Product name Field of application
DC70442 GRK6 inhibitor 18 GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
DC11955 Takeda compound 101 Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
DC73878 GRL018-21 GRL018-21 is a highly selective, potent, and non-covalent GRK5 inhibitor with IC50 of 10 nM, >100,000-fold selectivity over GRK2.
DC72121 CCG-273220 CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 220 nM. CCG-273220 is highly selective to GRK5 over GRK2 (IC50=350 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
DC71959 CCG-273463 CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 9 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer.
DC71958 CCG-271423 CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca2+ transience.
DC71670 KR-39038 KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.
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