| 应用 |
A selective inhibitor of ARK-1, ARK-2, and ARK-3. |
| 产品介绍 |
ZM 447439是一种选择性的，ATP竞争性Aurora A和Aurora B抑制剂，IC50分别为110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck选择性高8倍，对CDK1/2/4， Plk1， Chk1等几乎没有作用效果。 |
| 备注 |
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect againstCDK1/2/4, |
| 生化机理 |
ZM-447439 is a selective inhibitor of aurora kinases ARK-1 (A) (IC50=1000 nM, Ki=100nM), ARK-2 (B) (IC50= 50 nM, Ki= 0.36 nM) and ARK-3 (C), that can induce growth arrest, inhibit histone H3 phosphorylation and effectively activate apoptosis. The compound specifically interacts at the ATP-binding site and at the adjacent cleft, found only in aurora kinases. In the presence of Z-M447439, chromosome alignment, segregation, and cytokinesis during mitosis are unsuccessful. Studies show that ZM-447439 can override the spindle assembly checkpoint and accelerate meiosis I in mouse oocytes. |
| 别名 |
ZM447439; N-[4-[[6-甲氧基-7-[3-(4-吗啉基)丙氧基]-4-喹唑啉基]氨基]苯基]苯甲酰胺;ZM447439;ZM 447439;N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide |
