575545

XAV939

≥97% (HPLC), solid, Tankyrase1/2 inhibitor, Calbiochem

• 別名: Tankyrase1/2 Inhibitor, XAV939, 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V, TNKS1/2 Inhibitor I
• 実験式（ヒル表記法）: C₁₄H₁₁F₃N₂OS
• 分子量: 312.31
• UNSPSCコード: 12352200
• NACRES: NA.54

特性

• 製品名: Tankyrase1/2 Inhibitor, XAV939, The Tankyrase1/2 Inhibitor, XAV939 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 25 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

A cell-permeable dihydrothiopyranopyrimidinol that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (K_d = 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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Huang, S.M., et al. 2009. Nature461, 614.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H302
• 注意書き: P264 - P270 - P301 + P312 - P501
• 危険有害性の分類: Acute Tox. 4 Oral
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable