For research use only. Not for therapeutic Use.
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[1].
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].
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].
| Catalog Number | I044493 |
| CAS Number | 1144043-83-3 |
| Synonyms | disodium;[4-[[(6S,9aS)-1-(benzylcarbamoyl)-8-(1H-indazol-7-ylmethyl)-4,7-dioxo-2-prop-2-enyl-3,6,9,9a-tetrahydropyrazino[2,1-c][1,2,4]triazin-6-yl]methyl]phenyl] phosphate |
| Molecular Formula | C32H32N7Na2O7P |
| Purity | ≥95% |
| InChI | InChI=1S/C32H34N7O7P.2Na/c1-2-15-37-21-29(40)38-27(16-22-11-13-26(14-12-22)46-47(43,44)45)31(41)36(19-25-10-6-9-24-18-34-35-30(24)25)20-28(38)39(37)32(42)33-17-23-7-4-3-5-8-23;;/h2-14,18,27-28H,1,15-17,19-21H2,(H,33,42)(H,34,35)(H2,43,44,45);;/q;2*+1/p-2/t27-,28-;;/m0../s1 |
| InChIKey | BUCIVAHDHKFRLG-QLBXQKMFSA-L |
| SMILES | C=CCN1CC(=O)N2C(N1C(=O)NCC3=CC=CC=C3)CN(C(=O)C2CC4=CC=C(C=C4)OP(=O)([O-])[O-])CC5=CC=CC6=C5NN=C6.[Na+].[Na+] |
| Reference | [1]. Masibag AN, Bergin CJ, Haebe JR, et al. Pharmacological targeting of Sam68 functions in colorectal cancer stem cells. iScience. 2021;24(12):103442. |
