LF3

LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC₅₀ of 1.65 μM^[1]. IC50 & Target:IC50: 1.65 μM (β-Catenin/TCF4, AlphaScreen), 1.82 μM (β-Catenin/TCF4, ELISA)^[1] In Vitro:LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners^[1]. In Vivo:LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFP^high cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice^[1].