YB-0158 (Wnt pathway inhibitor 2) is a potent peptidomimetic compound that targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. As a reverse-turn agent, it induces apoptosis in CRC cells and exhibits strong anti-cancer activity.

Wnt:6.2 μM (IC50)

YB-0158, at concentrations of 0.2 μM and 0.5 μM over a 48-hour period, significantly enhances apoptosis in CRC cells, as evidenced by activated Caspase-3/7 detection assays[1]. Additionally, a 0.3 μM concentration of YB-0158 markedly reduces CBP recruitment at the LGR5 and MYC promoter regions of Wnt/beta-Catenin target genes in HT29 cells, compared to a DMSO control[1].

YB-0158 exhibits an effective concentration (EC 50) of 1.64 μM in MC38 cells cultured in vitro. In vivo experiments utilizing C57BL/6 mice with MC38 cell-derived tumors demonstrate that YB-0158 administered intraperitoneally (IP) at a dose of 100 mg/kg does not significantly alter primary tumor size compared to saline-treated controls[2].