TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

TCF4/β-catenin-IN-1 exhibits cytotoxic activity against HCT-116, A549, and HepG2 cancer cell lines with IC50 values of 8.52 μM, 5.87 μM, and 3.12 μM, respectively (0.4-100 μM, 24 h) [1]. At a concentration of 8.52 μM for 24 hours, it notably increases the expression levels of p53 and pro-apoptotic Bax, while reducing anti-apoptotic Bcl-2 expression in the HCT-116 cell line [1]. Additionally, TCF4/β-catenin-IN-1 inhibits the expression of β-catenin and TCF-4 in HCT-116 cells in a dose-dependent manner (5-20 μM) [1]. It also significantly upregulates the expression of caspase-3, caspase-8, and caspase-9 in the HCT-116 cell line at 8.52 μM [1]. Furthermore, TCF4/β-catenin-IN-1 inhibits CYP3A4, CYP1A2, and CYP2C19 [1].