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WIKI4 is a potent inhibitor of Wnt/β-catenin signaling with an EC50 ~ 75 nM in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U2OS osteosarcoma cells, and hESCs. WIKI4 inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) with an IC50 of 15 nM, preventing the ubiquitination and degradation of axin and thereby antagonizing Wnt signalling.
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