| 产品描述： | Wnt/β-连环蛋白抑制剂;Wnt/beta-catenin Inhibitors;;InformationLF3 LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.Targetsβ-catenin/Tcf4 (Cell-free assay) 1.65 μMIn vitroLF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. The self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. LF3 inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion. LF3 blocks the expression of a series of Wnt target genes in Wnt-addicted colon cancer cells. It inhibits proliferation of Wnt-addicted colon cancer cells through induction of cell-cycle arrest and also inhibits self-renewal capacity of CSCs.In vivoLF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer while exhibiting no significant toxicity for mice and does not disturb the normal histology of the gut of mice.Cell Research(from reference)Cell lines：The cell lines HCT116, HCT15, HT29, SW480, SW620, LS174T, SW48, MCF7, HeLa, HEK293, and MDCK\xa0 Concentrations：3.3-60 μmol/L Incubation Time：24 h |
| 靶点： |
IC50: 1.65 μM (β-Catenin/TCF4, AlphaScreen), 1.82 μM (β-Catenin/TCF4, ELISA) |
| 体内研究： |
LF3 可减缓小鼠结肠癌异种移植模型中的肿瘤生长并诱导分化。当用 50 mg/kg 的 LF3 治疗 GFPhigh 细胞的小鼠时，肿瘤生长显著减少。LF3 治疗不会扰乱小鼠肠道的正常组织学。 |
| 参考文献： |
1. Fang L, et al. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.401 ml |
12.003 ml |
24.006 ml |
| 5 mM |
0.48 ml |
2.401 ml |
4.801 ml |
| 10 mM |
0.24 ml |
1.2 ml |
2.401 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京