S89088 |
MSAB |
MedMol | 98% |
- 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。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)