Drug intelligence / Profile preview

MS115

Development stage
Preclinical
Lead developer
Icahn School of Medicine
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

MS115 is a potent and selective degrader of Protein Arginine Methyltransferase 5 (PRMT5) and its coactivator MEP50 (WD repeat-containing protein 77). Developed by researchers at the Icahn School of Medicine at Mount Sinai, MS115 is a proteolysis-targeting chimera (PROTAC) that leverages the ubiquitin-proteasome system to induce the degradation of the PRMT5/MEP50 complex. In preclinical studies, MS115 has demonstrated superior antiproliferative activity in breast and prostate cancer cell lines compared to traditional PRMT5 inhibitors and earlier-generation degraders. It is characterized by a favorable safety profile in normal cells, although it retains activity in MTAP-proficient cells. MS115 serves as both a high-quality chemical probe for studying PRMT5 biology and a lead candidate for the development of targeted therapies for PRMT5-dysregulated malignancies.

02

Targets

MEP50 (Methylosome protein 50)PRMT5 (Protein arginine N-methyltransferase 5)

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