CAY10574 |
| Catalog No.GC43175 |
CAY10574 es un potente inhibidor de CDK9/ciclina T1 competitivo con ATP con una IC50 de 0,35 μM. CAY10574 exhibe una selectividad de 38 veces para CDK9/ciclina T sobre otros complejos de CDK/ciclina. Actividad antitumoral.
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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.
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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