A cell-permeable inhibitor of Cdk1 and Cdk2
BMS265246 is a potent and selective inhibitor for CDK1 and CDK2 (IC50= 6 nM and 9 nM)
Cyclin-dependent kinases (CDK) are a group of serine/threonine kinases. They are activated by coupling to cyclin and participate in the regulation of cell cycle.
BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 μM and 0.76 μM) [1]. In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 μm—0.492 μm). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells. [2]
参考文献:
1. Misra RN, Xiao Hy, Rawlins DB et al.? 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.? Bioorg
Med Chem Lett.? 2003 Jul 21;13(14):2405-8.
2. Sutherland JJ, Low J, Blosser W et al.? A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.
| Cell experiment [1]: | |
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Cell lines |
HCT-116 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.293 ~ 0.492 μM |
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Applications |
In HCT-116 cells, BMS265246 blocked the cell proliferation with EC50 values ranging from 0.293 to 0.492 μM. Compared with R-547 group, BMS265246 group had a higher proportion of G2-apoptotic cells. BMS265246 treatment resulted in low DNA intensity, large round nuclei and 4N DNA content in the dominant cell population-G2 arrested cells. |
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参考文献: [1]. Sutherland JJ, Low J, Blosser W et al. A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54. | |
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