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Tankyrase1/2 Inhibitor, XAV939-Calbiochem
| 产品编号： | 4090932 |
| 规格： | The Tankyrase1/2 Inhibitor, XAV939 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
Tankyrase1/2 Inhibitor, XAV939-Calbiochem
2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V, TNKS1/2 Inhibitor I
基本信息
| Empirical Formula【经验(实验)分子式】 | C14H11F3N2OS |
| Molecular weight | 312.31 |
| General description【一般描述】 | A cell-permeable dihydrothiopyranopyrimidinol that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (Kd = 99 and 93 nM, respectively) and potently inhibits their PARsylation (poly ADP-ribosylation) activity (IC50 = 11 and 4 nM, respectively), while exhibiting much lower activity against PARP1 and PARP2 (IC50 = 2.194 and 0.114 µM, respectively). TNKS, but not PARP1/2, function knockdown by siRNA or XAV939 treatment suppresses cellular axin1/2 PARsylation and ubiquitination/proteasomal degradation, resulting in axin build-up, β-catenin destruction, and blockage of Wnt signaling. XAV939 is shown to inhibit the growth of β-catenin-dependent DLD-1, but not that of β-catenin-independent RKO, cells (by >95% vs. no effect at 3.3 µM, respectively) in vitro and prevent the regeneration of zebrafish tail fin (by ~70% at 7 d post-amputation, 5 µM) after surgical removal in vivo. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Huang, S.M., et al. 2009. Nature461, 614. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 25 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
