| Name | OSMI-1 |
| Description | OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans. |
| In vitro | METHODS: COS7 and Hela cells were treated with OSMI-1 (2-100 µM) for 24 h. Cell viability was measured using the CCK8 Assay.
RESULTS: 50 µM OSMI-1 reduced cell viability by more than 50%. [1]
METHODS: CHO cells were treated with OSMI-1 (10-100 µM) for 24 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: OSMI-1 reduced global OGlcNAcylation in a dose-dependent manner, with a maximum effect at 50 µM. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, OSMI-1 (1 mg/kg, i.v.) and TRAIL (500 µg/kg, intraperitoneally) were administered to BALB/c-Foxn1nu/ArcGem nude mice harboring human colorectal carcinoma tumor HCT116 once daily for three weeks.
RESULTS: Tumor size was slightly reduced in mice treated with OSMI-1 or TRAIL alone, but significantly reduced in the OSMI-1 and TRAIL combination group. The combination treatment synergistically increased the antitumor activity of transplanted tumors in HCT116 nude mice. [3]
METHODS: To investigate the protective effect against Stx-mediated pathogenic responses, OSMI-1 (300-1000 µg/mouse in water containing 4.5% DMSO and 5% Tween 80) was injected intraperitoneally into Stx2a-attacked C57BL/6 mice once daily for seven days.
RESULTS: O-GlcNAc inhibition ameliorated the mortality and various disease symptoms induced by Stx2a exposure in mice, which was further enhanced by O-GlcNAc inhibition. [4] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.83 mg/mL (3.25 mM), Solution.
DMSO : 104 mg/mL (184.51 mM), Sonication is recommended.
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| Keywords | zebrafish | transferase | toxicity | OSMI-1 | OSMI1 | OSMI 1 | OGT | O-GlcNAcylation | O-GlcNAc transferase (OGT) | O-GlcNAc transferase | O-GlcNAc | mono- acylglycerol acyltransferase | mammalian | Inhibitor | inhibit | Diglyceride acyltransferase | Diacylglycerol acyltransferase | cell-permeable | Acyltransferase | acyl-CoA:cholesterol acyltransferase |
| Inhibitors Related | Alendronate sodium trihydrate | Serotonin hydrochloride | Serotonin | D(+)-Raffinose pentahydrate | 2,2'-Methylenebis(6-tert-butyl-4-methylphenol) | Risedronic Acid | Cyclandelate | Entacapone | CBHcy | 2-Furoic acid | Flopropione | Tolcapone |
| Related Compound Libraries | Bioactive Compound Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max |
United States
