TargetMol

CMPD101

Product Code:
 
TAR-T14989
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T14989-1mg1mg£119.00
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TAR-T14989-5mg5mg£173.00
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TAR-T14989-1mL1 mL * 10 mM (in DMSO)£177.00
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TAR-T14989-10mg10mg£237.00
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TAR-T14989-25mg25mg£406.00
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TAR-T14989-50mg50mg£574.00
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Further Information

Bioactivity:
CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.
CAS:
865608-11-3
Formula:
C24H21F3N6O
Molecular Weight:
466.468
Pathway:
Cell Cycle/Checkpoint; Cytoskeletal Signaling; GPCR/G Protein; Chromatin/Epigenetic; Stem Cells
Purity:
0.9901
SMILES:
Cn1c(CNc2cccc(c2)C(=O)NCc2ccccc2C(F)(F)F)nnc1-c1ccncc1
Target:
ROCK; GRK; PKC

References

1. Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990. 2. Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.