Inhibitor of canonical Wnt signaling (IC50
= 790 nM). Targets the β
-catenin destruction complex (GSK-3�/AXIN/APC). Increases AXIN2 and decreases active β
-catenin levels in colorectal cancer (CRC) cells. Also arrests cell cycle in G1
and inhibits proliferation of CRC cells in vitro
. Inhibits tumor growth and formation in mouse models.
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Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth.
Waaler et al.
Cancer Res., 2011;71:197