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PKF118-310 Catalog No.GC18291

An inhibitor of the Tcf4-β-catenin protein interaction

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 84-82-2 SDF Download SDF
Synonyms N/A
Chemical Name 1,6-dimethyl-pyrimido[5,4-e]-1,2,4-triazine-5,7(1H,6H)-dione
Canonical SMILES O=C1N(C)C(C2=NC=NN(C)C2=N1)=O
Formula C7H7N5O2 M.Wt 193.2
Solubility Water: 10 mg/ml Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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.