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XAV 939 is a small molecule and selective Wnt pathway transcription factor β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4nM for the inhibition of TNKS1 and TNKS2, respectively. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex and stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. Deregulated Wnt/b-catenin pathway activity has been implicated in many cancers. ^[1]

• Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling Shih-Min A. Huang,Yuji M. Mishina,et al. Nature 1 October 2009;461:614-620

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