| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
O-GlcNAc transferase (OGT)
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|---|---|
| ln Vitro |
OSMI-1 (the active component in the racemate) inhibits OGT with an IC50 of 2.7 uM in biochemical assays. In cell-based assays, OSMI-1 inhibits protein O-GlcNAcylation in several mammalian cell lines (e.g., HEK293T, HeLa) without qualitatively altering cell surface N- or O-linked glycans. The racemate likely exhibits similar in vitro activity but may have reduced potency compared to the pure active enantiomer.
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| ln Vivo |
No specific in vivo data for the racemate; however, the active OSMI-1 has been used in studies to investigate the role of O-GlcNAcylation in cellular processes, including cancer, neurodegeneration, and metabolic regulation. In vivo studies typically involve administration of OSMI-1 (10-50 mg/kg) to rodents via intraperitoneal injection to modulate O-GlcNAcylation levels in tissues.
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| Enzyme Assay |
The OGT enzyme inhibition assay uses recombinant human OGT (or OGT from other species) and a suitable peptide substrate (e.g., a peptide derived from casein kinase II or TAB1) in the presence of UDP-GlcNAc. The reaction is incubated at 37degC for 30-60 minutes in a buffer containing Tris-HCl, NaCl, and DTT. Product formation (O-GlcNAcylated peptide) is detected by either a fluorescence-based assay using a labeled UDP-GlcNAc analog (e.g., UDP-6AzGlcNAc) or by ELISA using an anti-O-GlcNAc antibody. Alternatively, a radiometric assay using [3H]-UDP-GlcNAc is used. IC50 values are calculated.
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| Cell Assay |
Mammalian cell lines (e.g., HEK293T, HeLa, CHO, or cancer cell lines) are cultured in DMEM with 10% FBS and antibiotics. Cells are treated with (Rac)-OSMI-1 or OSMI-1 (1-50 uM) for 24-72 hours. Protein O-GlcNAcylation levels are assessed by Western blotting using a specific anti-O-GlcNAc antibody (e.g., RL2 or CTD110.6). Total OGT activity in cell lysates is measured using a fluorescence-based OGT activity assay kit. Cell viability is assessed by MTT or CellTiter-Glo assays. Cell surface glycans are analyzed by lectin blotting or flow cytometry.
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| Animal Protocol |
For in vivo studies, the active OSMI-1 is typically formulated in a suitable vehicle (e.g., 5% DMSO in PBS, or 10% DMSO/40% PEG300/5% Tween 80/45% saline) and administered to rodents via intraperitoneal injection at doses ranging from 10-50 mg/kg, once daily for up to 14 days. Tissues (liver, brain, kidney) are harvested, and O-GlcNAcylation levels are measured by Western blot. Plasma and tissue concentrations can be measured by LC-MS/MS. The racemate may be used in comparator studies.
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| ADME/Pharmacokinetics |
No specific PK data for the racemate; for OSMI-1, in vivo pharmacokinetics have been reported in rodents. Following intraperitoneal administration, OSMI-1 achieves measurable plasma concentrations and distributes to tissues including brain. Half-life, Cmax, AUC, and clearance have been characterized. It is metabolized in the liver and excreted via bile and urine. Oral bioavailability is likely low, with IP being the preferred route.
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| Toxicity/Toxicokinetics |
No specific toxicity data for (Rac)-OSMI-1; the active OSMI-1 has been evaluated in preclinical studies and is generally well tolerated at doses up to 50 mg/kg (IP) for short-term (up to 14 days) in rodents. Long-term safety studies are not publicly available. As an OGT inhibitor, it may affect O-GlcNAcylation-dependent cellular processes, but overt signs of toxicity are not reported at therapeutic doses.
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| References | |
| Additional Infomation |
(Rac)-OSMI-1 (CAS: 2748153-92-4) is the racemic mixture of OSMI-1, a first-in-class OGT inhibitor. O-GlcNAcylation is a post-translational modification involved in numerous cellular processes, including transcription, signaling, and metabolism. OSMI-1 is a valuable research tool for studying O-GlcNAc biology, epigenetics, and cancer. The racemate is often used as a control to assess enantiomer-specific effects. Neither (Rac)-OSMI-1 nor OSMI-1 is approved for clinical use. Molecular formula: C2₈H3₈N4O₈. It is soluble in DMSO.
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| Exact Mass |
563.118
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|---|---|
| CAS # |
2748153-92-4
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| Related CAS # |
OSMI-1;1681056-61-0
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| PubChem CID |
129205732
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
39
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| Complexity |
1000
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1C(C(=O)N(CC2=CC=CO2)CC3=CC=CS3)NS(=O)(=O)C4=CC5=C(C=C4)NC(=O)C=C5
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| InChi Key |
IYIGLWQQAMROOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H25N3O6S2/c1-36-25-9-3-2-8-23(25)27(28(33)31(17-20-6-4-14-37-20)18-21-7-5-15-38-21)30-39(34,35)22-11-12-24-19(16-22)10-13-26(32)29-24/h2-16,27,30H,17-18H2,1H3,(H,29,32)
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| Chemical Name |
N-(furan-2-ylmethyl)-2-(2-methoxyphenyl)-2-[(2-oxo-1H-quinolin-6-yl)sulfonylamino]-N-(thiophen-2-ylmethyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (88.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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