PKF118-310

An inhibitor of the Tcf4-β-catenin protein interaction

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库存: 现货

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1mg

￥262.00

210.00

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5mg

￥1212.00

970.00

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10mg

￥2062.00

1650.00

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货号: ajci20824
CAS: 84-82-2
别名: 毒黄素,Xanthothricin; Toxoflavine; PKF-118-310
分子式: C7H7N5O2
分子量: 193.2
纯度: >98%
溶解度: Water: 10 mg/ml
储存: Store at -20°C
库存: 现货

Background

PKF118-310 is an inhibitor of the interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains. It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 uM). 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.