YB-0158

Names

[ Name ]:
YB-0158

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Wnt

[Target]

Wnt:6.2 μM (IC50)

[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 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].

[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.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds

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