β-Catenin/Tcf Inhibitor II, PKF118-310

A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC₅₀ = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC₅₀ = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Wei, W., et al. 2010. Int. J. Cancer126, 2426.
Lepourcelet, M., et al. 2004. Cancer Cell5, 91.

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