| 货号 | 18014-50mg |
| 描述 | The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells.1 Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM) with >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins.2,3 It induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death (GI50s = 22-82 nM in colon, pancreas, prostrate, and lung cancer cells in vitro).1 At 10 mg/kg, ispinesib produces tumor regression of breast cancer cell xenografts in mice.4 It has also been used to halt the growth of treatment-resistant glioblastoma tumor-initiating cells, to prevent tumor initiation and self-renewal of a cancer stem cell population (EC50 = 1.15 nM), and to reduce glioma cell invasion.5 |
| 别名 | SB-715992; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Good, J.A.D.,Skoufias, D.A., and Kozielski, F. Elucidating the functionality of kinesins: An overview of small molecule inhibitors. Seminars in Cell & Developmental Biology 22(9), 935-945 (2011). 2.Good, J.A.D.,Wang, F.,Rath, O., et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. Journal of Medicinal Chemistry 56, 1878-1893 (2015). 3.Wang, F.,Good, J.A.D.,Rath, O., et al. Triphenylbutanamines: Kinesin spindle protein inhibitors with in vivo antitumor activity. Journal of Medicinal Chemistry 55, 1511-1525 (2012). 4.Purcell, J.W.,Davis, J.,Reddy, M., et al. Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clinical Cancer Research 16(2), 566-576 (2010). 5.Venere, M.,Horbinski, C.,Crish, J.F., et al. The mitotic kinesin KIF11 is a driver of invasion, proliferation, and self-renewal in glioblastoma. Sci.Transl.Med. 7(304), 1-12 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 517.1 |
| 分子式 | C30H33ClN4O2 |
| CAS号 | 336113-53-2 |
| 稳定性 | ≥ 2 years |
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