Based on assays of the transcriptional complexes, several small molecules were first identified as Wnt inhibitors that inhibited CRC cell proliferation and interfered with β-catenin-mediated axis duplication in Xenopus embryos.13,14 Through cell-based transcriptional reporter assay screening, additional Wnt inhibitors were identified that works through inhibiting the interaction between β-catenin and TCF/LEF transcriptional complexes in CRC.15–18 Recently, several small-molecule Wnt inhibitors targeting the destruction complex composed of APC, Axin, GSK3β and other proteins were discovered. This evidence concerns the gene AXIN1 and colorectal carcinoma.