Wnt信號(hào)通路是一個(gè)復(fù)雜的蛋白質(zhì)作用網(wǎng)絡(luò)，其功能zui常見于胚胎發(fā)育和癌癥，但也參與成年動(dòng)物的正常生理過程。Wnt信號(hào)通路包括許多可調(diào)控Wnt信號(hào)分子合成的蛋白質(zhì)，它們與靶細(xì)胞上的受體相互作用，而靶細(xì)胞的生理反應(yīng)則來源于細(xì)胞和胞外Wnt配體的相互作用。

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

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