5.00556

Tankyrase1/2 Inhibitor V, WIKI4

• 别名: Tankyrase1/2 Inhibitor V, WIKI4, 2-(3-((4-(4-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)sulfanyl)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, Wnt Pathway Inhibitor XVIII, TNKS1/2 Inhibitor V
• 经验公式（希尔记法）: C₂₉H₂₃N₅O₃S
• CAS号: 838818-26-1
• 分子量: 521.59
• MDL编号: MFCD05885187
• UNSPSC代码: 12352200
• PubChem化学物质编号: 2984337
• NACRES: NA.77

属性

• 方案: ≥98% (HPLC)
• 质量水平: 100
• 表单: powder
• 效能: 15 nM IC₅₀
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: pale yellow
• 溶解性: DMSO: 5 mg/mL
• 储存温度: 2-8°C
• SMILES字符串: COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6
• InChI: 1S/C29H23N5O3S/c1-37-22-11-9-21(10-12-22)34-26(20-13-15-30-16-14-20)31-32-29(34)38-18-4-17-33-27(35)23-7-2-5-19-6-3-8-24(25(19)23)28(33)36/h2-3,5-16H,4,17-18H2,1H3
• InChI key: RNUXIZKXJOGYQP-UHFFFAOYSA-N

说明

一般描述

A cell-permeable triazole derivative that acts as a reversible TNKS inhibitor (IC₅₀ = 15 nM in cell-free TNKS2 auto-ribosylation assays) and selectively inhibits Wnt/β-catenin, but not NF-κB, TGFβ, or retinoic acid, signaling pathway-dependent reporter activity. Although structurally distinct from XAV939, both compounds are shown to induce basal axin1/2 protein accumulation in DLD1 colon cancer cells with mutant APC (2.5 µM; 2 to 4 h) and prevent Wnt3a-induced axin1 protein degradation and β-catenin accumulation in A375 melanoma cells (1 µM; and up to 24 h) with similar potency. Likewise, WIKI4 also effectively inhibits the Wnt/β-catenin pathway-dependent growth of DLD1 (37% and 67% inhibition of colony formation in 10 days, respectively, in the presence of 0.1 and 1 µM WIKI4).

生化/生理作用

Cell permeable: yes

Primary Target
TNKS2

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Followig reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

James, R.G., et al. 2012. PLoS. One.7, e50457.

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable