YB-0158 (Wnt pathway inhibitor 2) 是一种反向转肽模拟物和一种有效的结直肠癌干细胞 (CSC) 靶向剂。YB-0158 破坏 Sam68-Src 相互作用并诱导结直肠癌细胞凋亡。YB-0158 具有抗癌活性。
货号:ajcx35416
CAS:1144043-83-3
分子式:C32H32N7Na2O7P
分子量：703.59
溶解度:DMSO : 100 mg/mL (142.13 mM; Need ultrasonic)|H2O :< 0.1 mg/mL (ultrasonic;adjust pH to 1 with 1M HCl) (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[1]. Masibag AN, Bergin CJ, Haebe JR, et al. Pharmacological targeting of Sam68 functions in colorectal cancer stem cells. iScience. 2021;24(12):103442.