| Description | YB-0158 (Wnt pathway inhibitor 2) is a powerful peptidomimetic compound that effectively targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. This compound acts as a reverse-turn agent, inducing apoptosis in CRC cells and displaying strong anti-cancer activities. |
| In 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[1]. 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[1]. |
| In vivo | YB-0158 displays an EC 50 (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]. |
| Target activity | Wnt:6.2 μM (IC50) |
| Synonyms | Wnt pathway inhibitor 2, YB-0158 |
| molecular weight | 703.6 |
| Molecular formula | C32H3N7Na2O7P |
| CAS | 1144043-83-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Masibag AN, Bergin CJ, Haebe JR, et al. Pharmacological targeting of Sam68 functions in colorectal cancer stem cells. iScience. 2021;24(12):103442. |