PKF118-310

PKF118-310 is an inhibitor of the protein-protein interaction between T cell factor 4 (Tcf4) and beta-catenin that is produced by Actinomycete strains. It disrupts binding of beta-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM). PKF118-310 blocks appearance of the Tcf4 and beta-catenin complex bound to DNA in an EMSA assay. It reduces levels of the beta-catenin regulated proteins c-Myc and cyclin D1 but has no effect on cyclin E in HCT116 cells. PKF118-310 (0.5 pmol) abrogates beta-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.Formal Name: 1,6-dimethyl-pyrimido[5,4-e]-1,2,4-triazine-5,7(1H,6H)-dione. CAS Number: 84-82-2. Synonyms: NSC 67078, Toxoflavin. Molecular Formula: C7H7N5O2. Formula Weight: 193.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Water: 10 mg/ml. lambdamax: 259, 396 nm. SMILES: O=C1N(C)C(C2=NC=NN(C)C2=N1)=O. InChi Code: InChI=1S/C7H7N5O2/c1-11-6(13)4-5(10-7(11)14)12(2)9-3-8-4/h3H,1-2H3. InChi Key: SLGRAIAQIAUZAQ-UHFFFAOYSA-N.