Drug intelligence / Profile preview

YL-109

Development stage
Preclinical
Lead developer
University of Tsukuba
Modality
Small Molecules
Administration
Intraperitoneal, Subcutaneous
01

Overview

YL-109 (2-(4-hydroxy-3-methoxyphenyl)-benzothiazole) is a novel small-molecule antitumor agent that acts as an activator of the carboxyl terminus of Hsp70-interacting protein (CHIP), also known as STUB1. It exerts its effects by activating the aryl hydrocarbon receptor (AhR) signaling pathway, which recruits AhR to the promoter region of the CHIP gene, thereby inducing CHIP transcription. In preclinical models, YL-109 has demonstrated the ability to inhibit cell growth, motility, and invasiveness in breast cancer, particularly triple-negative breast cancer (TNBC), and to suppress cancer stem cell properties. Additionally, it has shown protective effects in preclinical models of cisplatin-induced acute kidney injury and endometriosis by regulating CHIP-mediated protein degradation pathways.

Other names
2-(4-hydroxy-3-methoxyphenyl)-benzothiazole4-(1,3-benzothiazol-2-yl)-2-methoxyphenol4-(benzo[d]thiazol-2-yl)-2-methoxyphenolYP-109YP109YP 109
02

Targets

STUB1 (STIP1 homology and U-box-containing protein 1)AHR (Aryl hydrocarbon receptor)

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