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JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2 that blocks canonical Wnt signaling with an IC50 value of 790 nM.1,2 It increases the levels of Axin2 and decreases β-catenin levels in colorectal cancer (CRC) cells, leading to down-regulation of Wnt target genes.2 JW 74 inhibits the growth of CRC xenograft tumors in mice.2 JW 74 induces apoptosis and differentiation in osteosarcoma cell lines.1
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1. The tankyrase-
2. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 71(1), 197-205 (2011).