219331

β-Catenin/Tcf Inhibitor II, PKF118-310

The β-Catenin/Tcf Inhibitor II, PKF118-310 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Cancer applications.

• 別名: β-Catenin/Tcf Inhibitor II, PKF118-310, 1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
• 実験式（ヒル表記法）: C₇H₇N₅O₂
• 分子量: 193.16
• MDL番号: MFCD00459812
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: dark yellow
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC₅₀ = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC₅₀ = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) 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

Wei, W., et al. 2010. Int. J. Cancer126, 2426.
Lepourcelet, M., et al. 2004. Cancer Cell5, 91.

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: GHS06
• シグナルワード: Danger
• 危険有害性情報: H300
• 注意書き: P264 - P270 - P301 + P310 - P405 - P501
• 危険有害性の分類: Acute Tox. 2 Oral
• 保管分類コード: 6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable