WIKI4

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WIKI4  纯度: 99.93%

WIKI4 是一种有效的 tankyrase 抑制剂，其对 TNKS2 的 IC50 值为 26 nM。WIKI4 有效抑制 Wnt/β-catenin 信号传导，其 EC50 值为 75 nM。WIKI4 通过抑制 TNKS2 的酶活性来介导其对 Wnt/β-catenin 信号传导的影响。WIKI4 对 SCLC 细胞具有细胞毒性，其 IC50 值为 0.02 μM。

WIKI4

WIKI4 Chemical Structure

CAS No. : 838818-26-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥688 In-stock
5 mg ￥600 In-stock
10 mg ￥920 In-stock
25 mg ￥1850 In-stock
50 mg ￥3300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2[1][2]. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM[3].

IC50 & Target[2]

TNKS2

26 nM (IC50)

体外研究
(In Vitro)

WIKI4 (100 nM, 1 μM; 6 days; DLD1 cells) inhibits growth of DLD1 cells relative to DMSO controls in media containing low serum. WIKI4 inhibits expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling[1].
WIKI4 (1 μM; 2 hours, 4 hours, 6 hours, or 24 hours; DLD1 cells) significantly increases the steady-state abundance of AXIN1 and AXIN2[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: DLD1 cells
Concentration: 100 nM, 1 μM
Incubation Time: 6 days
Result: Inhibited growth of DLD1 cells.

Western Blot Analysis[1]

Cell Line: DLD1 cells
Concentration: 1 μM
Incubation Time: 2 hours,4 hours,6 hours, or 24 hours
Result: Significantly increased the steady-state abundance of AXIN1 and AXIN2.

分子量

521.59

Formula

C29H23N5O3S
CAS 号

838818-26-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 6.8 mg/mL (13.04 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9172 mL 9.5861 mL 19.1721 mL
5 mM 0.3834 mL 1.9172 mL 3.8344 mL
10 mM 0.1917 mL 0.9586 mL 1.9172 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. James RG, et al. WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling. PLoS One. 2012;7(12):e50457.

    [2]. Haikarainen T, et al. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4. PLoS One. 2013 Jun 6;8(6):e65404.

    [3]. Sadava D, et al. The effect of brassinolide, a plant steroid hormone, on drug resistant small-cell lung carcinoma cells. Biochem Biophys Res Commun. 2017 Nov 4;493(1):783-787.

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