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WIKI4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
WIKI4图片
CAS NO:838818-26-1
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
WIKI4 是一种有效的 tankyrase 抑制剂,对 TNKS2 的 IC50 为 26 nM。 WIKI4 有效抑制 Wnt/β-catenin 信号传导,其半数最大反应剂量为 75 nM。 WIKI4 通过抑制 TNKS2 的酶活性介导其对 Wnt/β-catenin 信号传导的影响。 WIKI4 对 SCLC 细胞具有细胞毒性,IC50 值为 0.02 μM。
Cas No.838818-26-1
化学名2-(3-((4-(4-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione
Canonical SMILESO=C1N(CCCSC2=NN=C(C3=CC=NC=C3)N2C4=CC=C(OC)C=C4)C(C5=CC=CC6=CC=CC1=C56)=O
分子式C29H23N5O3S
分子量521.59
溶解度≥ 26.1mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

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].

References:
[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.