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Beschreibung

A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts beta-catenin-Tcf4 interaction (IC50 = 0.8 µ,M in cell-free binding assays) and inhibits beta-catenin-regulated cellular transcription activity (IC50 = 0.3 µ,M in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse beta-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 beta-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.