113906-27-7

PNU 75654 (113906-27-7) disrupts the Wnt signaling pathway via inhibition of the interaction (KD50?= 450 nM) between β-catenin and T cell factor 4 (Tcf4).

PNU 74654 is a β-catenin inhibitor which inhibits interactions between β-catenin and transcription factor T-cell factor 4 (Tcf4) thus disrupting the Wnt signal transduction pathway.

PNU-74654 has been used:

• as a β-catenin signaling inhibitor to study its effects on the funnel cartilage differentiation in Sepia sp. embryos
• as a Wnt signaling inhibitor to study its effects on glycogen synthase kinase 3β (GSK-3β) inhibition in prostate cancer cell lines
• as a Wnt signaling inhibitor to study its effects on leptin-induced cell proliferation in breast cancer cells

PNU-74654 inhibits the Wnt-β catenin pathway by blocking the interaction between β-catenin and TCF (T cell factor). PNU-74654 is also an anti-tumor agent. Aberrant activation of the Wnt/β-catenin pathway (canonical pathway) is implicated in driving development/progression of different tumors, such as colon cancer, through interaction between β-catenin and T cell factor (TCF), which regulates the expression of target genes in cell proliferation and differentiation. Inhibition of this pathway activity in cancer cell lines efficiently blocks their growth. PNU-74654 inhibits this pathway by blocking the interaction between β-catenin and TCF.

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1) Trosset?et al. (2006)?Inhibition of protein-protein interactions: the discovery of druglike beta-catenin inhibitors by combining virtual and biophysical screening; Proteins,?64?60