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OSMI-1 is a quinolinone-6-sulfonamide that inhibits O-GlcNAc transferase (OGT; IC50 = 2.7 μM) in vitro.1 It is cell permeable and inhibits global O-GlcNAcylation in a dose-dependent manner in CHO cells. OSMI-1 induces a mass shift of nucleoporin62 (Nup62) that corresponds to the loss of O-GlcNAc residues and decreases levels of cellular O-GlcNAcase (OGA). OSMI-1 (50 μM) also causes a 50% decrease in CHO cell viability after 24 hours.
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1. A small molecule that inhibits OGT activity in cells. ACS Chem Biol. 10(6), 1392-1397 (2015).