XAV-939；XAV-02/10/50

产品信息

Wnt信号通路是一个复杂的蛋白质作用网络，其功能zui常见于胚胎发育和癌症，但也参与成年动物的正常生理过程。Wnt信号通路包括许多可调控Wnt信号分子合成的蛋白质，它们与靶细胞上的受体相互作用，而靶细胞的生理反应则来源于细胞和胞外Wnt配体的相互作用。

2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-one, is an inhibitor of Tankryases with IC50 of 11 and 4nM for Tankyrase 1 and Tankyrase 2, respectively. It stimulates beta-catenin degradation by stabilizing axin, resulting in the inhibition of the canonical WNT pathway. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. Tankryase inhibitors are potential therapeutics for cancers as deregulated Wnt/b-catenin pathway activity has been implicated in many cancers.

Purity:
Greater than 98% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.

Biological Activity:
In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 300 nM

重庆市华雅干细胞技术有限公司