PNU74654

PNU74654 is a small molecule inhibitor that specifically disrupts the interaction between β-catenin and T-cell factor (TCF) transcription factors, particularly TCF4. By binding to the armadillo repeat domain of β-catenin, it prevents the formation of the β-catenin/TCF complex, thereby inhibiting the transcription of Wnt signaling target genes. In the context of oncology research, it has been shown to suppress the activation of cancer-associated fibroblasts (CAFs) and reduce the expression of periostin (POSTN), which in turn sensitizes melanoma cells to targeted therapies like BRAF inhibitors. It is primarily used as a chemical probe in preclinical studies to investigate Wnt/β-catenin signaling pathways in various cancers, including colorectal and breast cancer.

Other names

5-methyl-2-phenyl-4-[(phenylamino)methyl]-2,4-dihydro-3H-pyrazol-3-one