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 or 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 ubiquitinproteasome pathway. Tankryase inhibitors are potential therapeutics for cancers as deregulated Wnt/b-catenin pathway activity has been implicated in many cancers.
Ref: Huang SM et al. Nature. 2009 Oct 1; 461(7264):614-20.
In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 300 nM.
CAS No.: 284028-89-3