Inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). Activity results in stabilization of Axin2 and increased degradation of β-catenin; inhibits the β-catenin signaling pathway. Also shown to decrease canonical Wnt signaling in SW480 and HCT-15 colon carcinoma cell lines; reduces cell cycle progression and proliferation in SW480 cells in vitro
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A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice.
Waaler et al.
Cancer Res., 2012;72:2822