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.

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

GB1874 is an inhibitor of the Wnt pathway targeting β-catenin-TCF4 protein-protein interaction (PPI), affecting proliferation and stemness in Wnt-dependent colorectal cancer (CRC) cells and inhibiting the growth of HCT116 tumour xenografts in vivo.

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)

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.

aStAx-35R TFA is a stapled peptide that antagonizes the nuclear form of β-catenin and inhibits Wnt signaling. It competitively inhibits the binding of β-catenin to TCF4. Furthermore, aStAx-35R TFA selectively induces growth inhibition in Wnt-dependent cancer cells.