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LF3 is a potent and selective small-molecule antagonist of the Wnt/β-catenin signaling pathway. It specifically targets and disrupts the protein-protein interaction between β-catenin and the transcription factor TCF4 (Transcription factor 7-like 2). By preventing the formation of this transcriptional complex, LF3 inhibits the expression of Wnt-responsive genes that are critical for cancer stem cell self-renewal, epithelial-mesenchymal transition (EMT), and metastatic outgrowth. In preclinical studies, LF3 has demonstrated the ability to reduce the burden of bone metastasis in breast and prostate cancer models by blocking the Wnt signaling activated by the bone vascular niche. It is widely utilized as a research tool to investigate the therapeutic potential of targeting the β-catenin/TCF interaction in various malignancies, including colorectal and breast cancers.
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