MSAB

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MSAB 是 Wnt/β-catenin 信号传导的选择性抑制剂。 MSAB 与 β-catenin 结合，促进其降解，并特异性下调 Wnt/β-catenin 靶基因。MSAB 对抗 Wnt/β-catenin 信号传导，并被鉴定为 Wnt/β-catenin 信号传导的选择性抑制剂。

MSAB is a selective inhibitor of Wnt/β-catenin signaling.?MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.MSAB act against Wnt/β-catenin signaling and identified ?as a selective inhibitor of Wnt/β-catenin signaling.?MSAB shows potent anti-tumor effects selectively on Wnt-dependent cancer cells in vitro and in mouse cancer models.?MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.?might represent an effective therapeutic strategy for cancers addicted to the Wnt/β-catenin signaling pathway.

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.

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. dailyfor 2 weeks Result:Reduced the size and weight of various types of Wnt-dependent HCT116, HT115, and H23 tumors.

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Wnt/Notch/Hedgehog

Wnt/beta/catenin

Wnt/β-catenin

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173436-66-3

305.35

C15H15NO4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (818.73 mM)

COC(=O)c1cccc(NS(=O)(=O)c2ccc(C)cc2)c1

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(-20℃)

With Ice Pack

≥ 2 years