MSAB

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[1].

MSAB (2-10 μM) selectively decreases cell viability of Wnt-dependent cells while showing little effect on Wnt-independent cells and normal human cells[1].MSAB (0.01-10 μM; 20 h) inhibits T-cell factor (TCF) luciferase reporter activity in HCT116 cells[1].MSAB (20 h) suppresses the Wnt3a-induced TOP-Luc activation and increases of active β-catenin levels in HEK293T cells[1].MSAB (0.5-10 μM; 20 h) decreases mRNA and protein levels of endogenous Wnt target genes in HCT116 cells[1].MSAB (5 μM; 16 h) induces degradation of β-catenin in a proteasome-dependent manner in HCT116 cells[1].

MSAB (10-20 mg/kg; i.p. daily for 2 weeks) inhibits tumor growth of Wnt-dependent cancer cells in mouse xenograft model[1].MSAB (10-20 mg/kg; i.p. twice daily for 2 weeks) inhibits tumor growth of MMTV-Wnt1 transgenic mice[1]. Animal Model: Athymic nude mice (5-6 weeks) are injected HCT116, HT115, H23, or H460 cells[1]

[1]. Hwang SY, et, al. 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.