| 货号 | 16873-1mg |
| 描述 | Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.1 MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.2,3,4 OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).5 It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.5 It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.5 OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jiang, P., and Zhang, D. Maternal embryonic leucine zipper kinase (MELK): A novel regulator in cell cycle control, embryonic development, and cancer. International Journal of Molecular Sciences 14(11), 21551-21560 (2013). 2.Gray, D.,Jubb, A.M.,Hogue, D., et al. Maternal embryonic leucine zipper kinase/murine protein serine-threonine kinase 38 is a promising therapeutic target for multiple cancers. Cancer Research 65(21), 9751-9761 (2005). 3.Joshi, K.,Banasavadi-Siddegowda, Y.,Mo, X., et al. MELK-dependent FOXM1 phosphorylation is essential for proliferation of glioma stem cells. Stem Cells 31(6), 1051-1063 (2013). 4.Nakano, I.,Joshi, K.,Visnyei, K., et al. Siomycin A targets brain tumor stem cells partially through a MELK-mediated pathway. Neuro.Oncol. 13(6), 622-634 (2011). 5.Chung, S.,Suzuki, H.,Miyamoto, T., et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget 3(12), 1629-1640 (2012). 6.Chung, S., and Nakamura, Y. MELK inhibitor, novel molecular targeted therapeutics for human cancer stem cells. Cell Cycle 12(11), 1655-1656 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 523.9 |
| 分子式 | C25H28Cl2N4O2 • HCl |
| CAS号 | 1431698-10-0 |
| 稳定性 | ≥ 2 years |
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