Drug intelligence / Profile preview

OSMI-4b

Development stage
Preclinical
Lead developer
Utrecht University
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
In Vitro (cell Culture Studies)
01

Overview

OSMI-4b is a potent, selective small molecule inhibitor of the enzyme O-linked N-acetylglucosamine transferase (OGT). It has an EC50 of approximately 3 μM in cells and is considered one of the most effective cell-active inhibitors for probing the biological functions of OGT. By inhibiting OGT, it reduces protein O-GlcNAcylation—a post-translational modification involved in numerous cellular processes including signaling, transcription regulation, and stress response. The compound was discovered through high-throughput screening and further optimized for potency. While highly useful as a research tool to study epigenetics and cell signaling pathways involving protein glycosylation, its physicochemical properties currently limit its development as a therapeutic drug candidate[1][3][5].

Other names
OGT inhibitor 4bOSMI 4OSMI4OSMI-4
02

Targets

OGT (UDP-N-acetylglucosamine—peptide N-acetylglucosaminyltransferase)

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