NU 6102 |
Katalog-Nr.GC18278 |
NU 6102 ist ein potenter CDK1- und CDK2-Inhibitor mit IC50-Werten von 9,5 nM bzw. 5,4 nM für CDK1/CyclinB und CDK2/CyclinA3. NU 6102 zeigt Selektivität für CDK1/CDK2 gegenüber CDK4 (IC50 von 1,6 μM), DYRK1A (IC50 von 0,9 μM), PDK1 (IC50 von 0,8 μM) und ROCKII (IC50 von 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.
Review for NU 6102
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(Based on Reviews and 17 reference(s) in Google Scholar.)Review for NU 6102
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