An inhibitor of the Tcf4-β-catenin protein interaction; disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM); blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay; reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 in HCT116 cells; reduces growth of HCT116

PKF118-310 – 10 mg

Brand:
Cayman
CAS:
84-82-2
Storage:
-20
UN-No:
- / 6.1

PKF118-310 is an inhibitor of the interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains.{40755} It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM). 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.{40756}  

 

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Description

An inhibitor of the Tcf4-β-catenin protein interaction; disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM); blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay; reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 in HCT116 cells; reduces growth of HCT116, HT-29, PC3, and DU145 cancer cells in vitro (IC50s = 170-300 nM); reduces tumor growth and expression of c-Myc, cyclin D1, and Survivin in a HepG2 mouse xenograft model (1 mg/kg twice per week)

Formal name: 1,6-dimethyl-pyrimido[5,4-e]-1,2,4-triazine-5,7(1H,6H)-dione

Synonyms:  NSC 67078|Toxoflavin

Molecular weight: 193.2

CAS: 84-82-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|Wnt Signaling

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