XAV939
货号：
13596-1mg 基本售价：
140.0 元 规格：
1 mg
产品信息
概述| 货号 | 13596-1mg |
| 描述 | The Wnt signaling pathway is integral to normal biological processes and inappropriately active in many cancers. It is regulated through degradation of the downstream effector β-catenin via a complex consisting of the tumor suppressor APC, axin, and glycogen synthase kinase 3 (GSK3). Axin is the concentration-limiting factor for this degradation complex. Initially indentified as telomere-associated proteins1, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation).2 XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively.2 By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.2 At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Smith, S.,Giriat, I.,Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282, 1484-1487 (1998).
2.Huang, S.M.A.,Mishina, Y.M.,Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461, 614-619 (2009).
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| 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 | 312.3 |
| 分子式 | C14H11F3N2OS |
| CAS号 | 284028-89-3 |
| 稳定性 | ≥ 2 years |
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