OSMI-3

OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells[1].

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

O-linked N-acetylglucosamine transferase (OGT)[1]

OSMI-3 (Compound 2b; 20-50 μM; 4-24 hours; HCT116 cells) treatment significantly reduces O-GlcNAc levels, and has more sustained cellular effects than OSMI-2[1]. A decrease in HCF-1 cleavage products and the appearance of uncleaved HCF-1 in cells treated with OSMI-3 (Compound 2b) is observed. Because OGT knockdown is known to decrease cell proliferation, the effects of OSMI-3 on cell growth in culture over 96h is also monitored. Although there is no evidence of apoptosis, the reduced growth of cells over time is observed, consistent with the knockdown results[1]. Western Blot Analysis[1] Cell Line: HCT116 cells Concentration: 20 μM, 40 μM, 50 μM Incubation Time: 4 hours, 24 hours Result: Reduced O-GlcNAc levels.

[1]. Martin SES, et al. Structure-Based Evolution of Low Nanomolar O-GlcNAc Transferase Inhibitors. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545.