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5mg |
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10mg |
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25mg |
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50mg |
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Purity: ≥98%
OSMI-1 (OSMI1; OSMI 1) is a novel, potent, cell permeable and quinolinone-6-sulfonamide-based inhibitor of O-GlcNAc transferase (OGT) with an IC50 value of 2.7 μM. 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.
ln Vitro |
After treatment for 24 hours, OSMI-1 (50 μM; CHO cells) decreases viability by about 50% [1]. Treatment with OSMI-1 (10-100 μM; 24 hours; CHO cells) decreased O-GlcNAcylation (global O-linked N-acetylglucosamine) in a dose-dependent manner. OGT activity in cells is inhibited by OSMI-1 [1].
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ln Vivo |
Mammals and zebrafish share remarkably comparable toxicity profiles; in fact, zebrafish are frequently used as a transitional species between conventional animal testing and cell-based evaluations. The in vivo acute toxicity of OSM1-1 was investigated using a zebrafish model. The LC50 values for OSM1-1 in the zebrafish model are 0.031 mg/mL (56 μM, 12 hours) and 0.025 mg/mL (45 μM, 24 hours) [2].
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Cell Assay |
Cell viability assay [1]
Cell Types: CHO Cell Tested Concentrations: 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Viability diminished by approximately 50% after 24 hrs (hours). Western Blot Analysis[1] Cell Types: CHO Cells Tested Concentrations: 10 μM, 25 μM, 50 μM, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Overall OGlcNAc acylation was diminished in a dose-dependent manner. |
References |
[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. |
Molecular Formula |
C28H25N3O6S2
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Molecular Weight |
563.644604444504
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CAS # |
1681056-61-0
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Related CAS # |
(Rac)-OSMI-1;2748153-92-4
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SMILES |
O=C(N(CC1=CC=CO1)CC2=CC=CS2)[C@@H](C3=CC=CC=C3OC)NS(=O)(C4=CC5=C(NC(C=C5)=O)C=C4)=O
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InChi Key |
IYIGLWQQAMROOF-HHHXNRCGSA-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)/t27-/m1/s1
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Chemical Name |
(R)-N-(Furan-2-ylmethyl)-2-(2-methoxyphenyl)-2-(2-oxo-1,2-dihydroquinoline-6-sulfonamido)-N-(thiophen-2-ylmethyl)acetamide
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Synonyms |
OSMI1 OSMI 1 OSMI-1
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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 : ~100 mg/mL (~177.42 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.69 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | |
5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | |
10 mM | 0.1774 mL | 0.8871 mL | 1.7742 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.