NU6140 |
| カタログ番号GC34692 |
NU6140 は選択的 CDK2-サイクリン A 阻害剤 (IC50、0.41 μM) であり、他の CDK よりも 10 ～ 36 倍の選択性を示します。 NU6140 はまた、それぞれ 67 および 35 nM の IC50 で、Aurora A および Aurora B を強力に阻害します。抗がん作用により、アポトーシス効果を高めます。
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Cas No.: 444723-13-1
Sample solution is provided at 25 µL, 10mM.
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NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively[2]. Anti-cancer activity[1][2]. cdk2-cyclin A|0.41 μM (IC50)|CDK1-Cyclin B|6.6 μM (IC50)|CDK4-Cyclin D|5.5 μM (IC50)|cdk5-p25|15 μM (IC50)|cdk7-cyclin H|3.9 μM (IC50)|Aurora A|67 nM (IC50)|Aurora B|35 nM (IC50)
NU6140 is less active on CDK1-cyclin B, CDK4-cyclin D, CDK5-p25 and CDK7-cyclin H, with IC50s of 0.41, 6.6, 5.5, 15 and 3.9 μM, respectively[1].NU6140 increases catalytic activity of capase-9 and capase-3, causes increase in the sub-G1 apoptotic cell population[1].
[1]. Pennati M, et al. Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37.
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