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CAS No.: 838818-26-1

WIKI4 Catalog No. CSN15823

Synonyms: Tankyrase 1/2 Inhibitor V

WIKI4 is a potent inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM) and inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM).

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技术信息

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IC50:~15nM
描述The Wnt/ß-catenin signaling pathway controls important cellular events during development and often contributes to disease when dysregulated. Tankyrases are enzymes catalyzing a covalent modification of proteins, poly(ADP-ribosyl)ation or PARsylation and are a part of the ß-catenin destruction complex. WIKI4 is a potent inhibitor of Wnt/β-catenin signaling with EC₅₀ ~ 75 nM and inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) with IC₅₀ ~15 nM. WIKI4 was cytotoxic to small-cell lung carcinoma cells with IC₅₀ of 0.02 µM^[3]. Overnight treatment of WIKI4 at 2.5 mM inhibited ubiquitylation of AXIN2 in SW480 colorectal carcinoma cells^[4].
作用机制WIKI4 inhibits TNKS2 mainly by interacting with His1048 and Phe1035 which are unique for tankyrases.
参考文献

[1] Haikarainen T, Venkannagari H, et al. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4. PLoS One. 2013 Jun 6;8(6):e65404.
[2] James RG, Davidson KC, et al. WIKI4, a novel inhibitor of tankyrase and Wnt/S-catenin signaling. PLoS One. 2012;7(12):e50457.
[3] Sadava D, Kane SE. 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. doi: 10.1016/j.bbrc.2017.08.094. Epub 2017 Aug 25. PMID: 28847728.
[4] James RG, Davidson KC, Bosch KA, Biechele TL, Robin NC, Taylor RJ, Major MB, Camp ND, Fowler K, Martins TJ, Moon RT. WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling. PLoS One. 2012;7(12):e50457. doi: 10.1371/journal.pone.0050457. Epub 2012 Dec 5. PMID: 23227175; PMCID: PMC3515623.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9172 mL
- 9.5861 mL
- 19.1722 mL
- 5 mM
- 0.3834 mL
- 1.9172 mL
- 3.8344 mL
- 10 mM
- 0.1917 mL
- 0.9586 mL
- 1.9172 mL

技术信息

CAS号

838818-26-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H23N5O3S

运输

蓝冰

分子量

521.59

别名

Tankyrase 1/2 Inhibitor V

溶解度

DMSO	7.0 mg/mL (13.4 mM) warming
Water	Insoluble
Ethanol	Insoluble

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