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575545 Tankyrase1/2 Inhibitor, XAV939 - Calbiochem

概述

重要规格表

Empirical Formula
C₁₄H₁₁F₃N₂OS

价格及供货情况

产品目录编号 库存情况包装 数量 / 包装 价格 数量
575545-10MGCN
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      Description
      OverviewA 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.
      Catalogue Number575545
      Brand Family Calbiochem®
      SynonymsTNKS1/2 Inhibitor I, 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V
      References
      ReferencesHuang, S.M., et al. 2009. Nature 461, 614.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₄H₁₁F₃N₂OS
      Chemical formulaC₁₄H₁₁F₃N₂OS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥97% by HPLC
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      产品目录编号 GTIN
      575545-10MGCN 04055977189261