tcf4/β-catenin

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.

PNU 74654 binds to β-catenin (Kd = 450 nM), inhibiting its interaction with the transcription factor T cell factor 4 (Tcf4) resulting in disruption of the Wnt signaling pathway.

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 (IC50 < 2 μM)

Toxoflavin (Xanthothricin) is an antagonist of the transcription factor 4 (TCF4) β-catenin complex and also inhibits KDM4A.

BC21, a β-catenin Tcf4 inhibitor, efficiently blocks the interaction between β-catenin and peptides derived from Tcf4, and diminishes the activity of β-catenin Tcf4-driven reporter genes. This compound has applications in cancer research.