| Bioactivity | OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans[1][2]. | ||||||||||||
| Target | IC50: 2.7 μM (O-GlcNAc transferase) | ||||||||||||
| Invitro | OSMI-1 (50 μM; 24 hours; CHO cells) treatment decreases the viability by about 50% after 24 hours[1].OSMI-1 (10-100 μM; 24 hours; CHO cells) treatment reduces global O-linked N-acetylglucosamine (O-GlcNAcylation) a dose-dependent manner. OSMI-1 inhibits OGT activity in cells[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | Mammalian and zebrafish toxicity profiles are strikingly similar, and zebrafish can usually serve as an intermediate step between cell-based evaluation and conventional animal testing. 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]. | ||||||||||||
| Name | OSMI-1 | ||||||||||||
| CAS | 1681056-61-0 | ||||||||||||
| Formula | C28H25N3O6S2 | ||||||||||||
| Molar Mass | 563.64 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ortiz-Meoz RF, et al. A small molecule that inhibits OGT activity in cells. ACS Chem Biol. 2015 Jun 19;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 Sep 26;7(1):12334. |