CAY10574 |
| Catalog No.GC43175 |
CAY10574 est un puissant inhibiteur de CDK9/cycline T1 compétitif pour l'ATP avec une IC50 de 0,35 μM. CAY10574 présente une sélectivité de 38 fois pour CDK9/cycline T par rapport aux autres complexes CDK/cycline. Activité antitumorale.
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Cas No.: 140651-18-9
Sample solution is provided at 25 µL, 10mM.
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Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value of 0.35 µM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively. CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively.
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