NU 6102 |
Catalog No.GC18278 |
NU 6102 est un puissant inhibiteur de CDK1 et CDK2 avec des IC50 de 9,5 nM et 5,4 nM pour CDK1/cyclinB et CDK2/cyclinA3, respectivement. NU 6102 montre une sélectivité pour CDK1/CDK2 sur CDK4 (IC50 de 1,6 μM), DYRK1A (IC50 de 0,9 μM), PDK1 (IC50 de 0,8 μM) et ROCKII (IC50 de 0,6 μM).
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Cas No.: 444722-95-6
Sample solution is provided at 25 µL, 10mM.
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. NU 6102 is a potent inhibitor of Cdk1 and Cdk2 with Ki values of 9 and 6 nM and IC50 values of 9.5 and 5.4 nM, respectively. NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2. Time-lapse videomicroscopy reveals that 20 μM NU 6102 delays cell entry into mitosis where most cells appear to eventually complete mitotic division but cannot correctly undergo cytokinesis, and hence become binucleated with an abnormal number of centrosomes. In SKUT-1B cancer cells a 24 h exposure to NU 6102 induced G2 arrest, inhibition of target protein phosphorylation, and cytotoxicity with an LC50 value of 2.6 μM.
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