N‐acetylglucosamine (O‐GlcNAc) residues is catalyzed by O‐GlcNAc transferase (OGT). O‐
GlcNAc is conserved within mammals and is implicated in a wide range of physiological
processes. Herein, we describe metabolic precursor inhibitors of OGT suitable for use both
in cells and in vivo in mice. These 5‐thiosugar analogues of N‐acetylglucosamine are
assimilated through a convergent metabolic pathway, most likely involving N …