YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities.IC50 & Target: Wnt signalingIn Vitro: YB-0158 (0.2 μM and 0.5 μM; 48 hours) significantly increases apoptosis in CRC cells as represented by activated Caspase-3/7 detection assays.
YB-0158 (0.3 μM) similarly decreases CBP recruitment at the promoter of Wnt/beta-Catenin target genes LGR5 and MYC in HT29 cells, compared with DMSO control.In Vivo: YB-0158 displays an EC50 (1.64 μM) in cultured MC38 cells. YB-0158 (100 mg/kg; IP; C57BL/6 mice bearing MC38 cells) shows no significant differences in primary tumor size in vivo treatments versus saline controls[2].