| 产品描述: | MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells |
| 靶点: |
Wnt/β-catenin;Wnt/beta-catenin |
| 体外研究: |
MSAB (2-10 μM) selectively decreases cell viability of Wnt-dependent cells while showing little effect on Wnt-independent cells and normal human cells. MSAB (0.01-10 μM; 20 h) inhibits T-cell factor (TCF) luciferase reporter activity in HCT116 cells. MSAB (20 h) suppresses the Wnt3a-induced TOP-Luc activation and increases of active β-catenin levels in HEK293T cells. MSAB (0.5-10 μM; 20 h) decreases mRNA and protein levels of endogenous Wnt target genes in HCT116 cells. MSAB (5 μM; 16 h) induces degradation of β-catenin in a proteasome-dependent manner in HCT116 cells. |
| 体内研究: |
MSAB (10-20 mg/kg; i.p. daily for 2 weeks) inhibits tumor growth of Wnt-dependent cancer cells in mouse xenograft model. MSAB (10-20 mg/kg; i.p. twice daily for 2 weeks) inhibits tumor growth of MMTV-Wnt1 transgenic mice. Animal Model: Athymic nude mice (5-6 weeks) are injected HCT116, HT115, H23, or H460 cells Dosage: 10, 20 mg/kg Administration: I.p. daily for 2 weeks Result: Reduced the size and weight of various types of Wnt-dependent HCT116, HT115, and H23 tumors. |
| 参考文献: |
1. Hwang SY, Deng X, Byun S, Lee C, Lee SJ, Suh H, Zhang J, Kang Q, Zhang T, Westover KD, Mandinova A, Lee SW. Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling. Cell Rep. 2016 Jun 28;16(1):28-36. doi: 10.1016/j.celrep.2016.05.071. Epub 2016 Jun 16. PubMed PMID: 27320923; PubMed Central PMCID: PMC4957947. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.275 ml |
16.375 ml |
32.749 ml |
| 5 mM |
0.655 ml |
3.275 ml |
6.55 ml |
| 10 mM |
0.327 ml |
1.637 ml |
3.275 ml |
| 50 mM |
0.065 ml |
0.327 ml |
0.655 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。 |