XAV-939; 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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