PKF118-310

PKF118-310 is an inhibitor of the protein-protein interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains.¹ It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC₅₀ = 0.8 µM). PKF118-310 blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay. It reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 but has no effect on cyclin E in HCT116 cells. PKF118-310 (0.5 pmol) abrogates β-catenin, but not siamois, ventral body axis duplication induced by mRNA in Xenopus embryos. It reduces growth of HCT116, HT-29, PC3, and DU145 cancer cells in vitro (IC₅₀s = 170-300 nM). PKF118-310 (1 mg/kg twice per week) reduces tumor growth and expression of c-Myc, cyclin D1, and Survivin in a HepG2 mouse xenograft model.²

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1. Lepourcelet, M., Chen, Y.N., France, D.S., et al. Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex. Cancer Cell 5(1), 91-102 (2004).

2. Wei, W., Chua, M.-S., Grepper, S., et al. Small molecule antagonists of the Tcf4/β-catenin complex inhibit the growth of HCC cells in vitro and in vivo. Int. J. Cancer 126(10), 2426-2436 (2010).