XAV939

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Description

XAV939 is an inhibitor of Tankryases with IC50 values 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. Wnt proteins act on a variety of stem cells that include neural, mammary and embryonic stem cells. XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. In addition, XAV939 inhibits growth of DLD-1 cells, an APC-deficient colorectal cancer cell line.

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