OSMI-1

SKU: orb1307925

Description

OSMI-1 is a cell-permeable, orally bioavailable small molecule inhibitor of O-GlcNAc transferase (OGT) with an IC50 of 2.7 µM. It selectively reduces protein O-GlcNAcylation in cellular and in vivo models without broadly affecting other glycosylation pathways, making it a valuable research tool for studying nutrient sensing, cellular stress, and transcriptional regulation.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1681056-61-0
• MW: 563.64
• Purity: 99.83% (May vary between batches)
• Formula: C₂₈H₂₅N₃O₆S₂
• SMILES: O=C(N(CC1=CC=CS1)CC2=CC=CO2)[C@@H](C3=C(C=CC=C3)OC)NS(=O)(C4=CC=C(NC(C=C5)=O)C5=C4)=O
• Target: Acyltransferase,Transferase
• Solubility: DMSO:104 mg/mL (184.51 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1.83 mg/mL (3.25 mM)

Bioactivity

• Target IC50:
  CHO cells:50 μM|OGT:2.7 μM
• 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. 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.
  Read more...
• 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%. 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Diglyceride acyltransferase, Diacylglycerol acyltransferase, cell-permeable, acyl-CoA:cholesterol acyltransferase, Acyltransferase, Inhibitor, inhibit, OSMI 1, OSMI1, OSMI-1, O-GlcNAc, O-GlcNAc transferase, O-GlcNAc transferase (OGT), O-GlcNAcylation, OGT, mono- acylglycerol acyltransferase, mammalian, toxicity, zebrafish, transferase

Compound Identifiers

PubChem CID

129205732