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Overview
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Background
OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM, it is cell permeable[1].
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[1].
The zebrafish model is used to investigate OSM1-1 acute toxicity in vivo. The LC50 of OSM1-1 is 0.031 mg/mL (56 μM, 12 h) and 0.025 mg/mL (45 μM, 24 h) in zebrafish model[2].[1]. Ortiz-Meoz RF, et al. A small molecule that inhibits OGT activity in cells. ACS Chem Biol, 2015, 10(6): 1392-7.
[2]. Liu Y, et al. Discovery of a Low Toxicity O-GlcNAc Transferase (OGT) Inhibitor by Structure-based Virtual Screening of Natural Products. Sci Rep, 2017, 7(1): 12334.
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