Abstract: Provided herein are O-GlcNAc transferase (OGT) inhibitor compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., diabetes and complications thereof, neurodegenerative diseases, proliferative diseases such as cancers, autoimmune diseases, and inflammatory diseases) in a subject. Provided are methods of inhibiting OGT in a subject or biological sample.

Abstract: The present invention provides inhibitors of O-GlcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, metabolic diseases, neurodegenerative diseases, proliferative diseases (e.g., cancers), autoimmune diseases, and inflammatory diseases.