PKF118-310 (Xanthothricin) 是转录因子 4 (TCF4)/β-catenin complex 的拮抗剂，也可作为 KDM4A 的抑制剂，具有抗肿瘤活性。
| Cas No. |
84-82-2 |
| 别名 |
毒黄素,Xanthothricin; Toxoflavine; PKF-118-310 |
| 化学名 |
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 |
| 分子式 |
C7H7N5O2 |
| 分子量 |
193.2 |
| 溶解度 |
Water: 10 mg/ml |
| 储存条件 |
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. |
| Shipping Condition |
Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 半岛bd体育手机客户端 描述 |
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. |
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