1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. OSMI-2

OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.

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OSMI-2 Chemical Structure

OSMI-2 Chemical Structure

CAS No. : 2260542-60-5

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5 mg USD 170 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells[1].

IC50 & Target

O-linked N-acetylglucosamine transferase (OGT)[1]

In Vitro

OSMI-2 (Compound 1b; 20-50 μM; 4-24 hours; HCT116 cells) treatment reduces O-GlcNAc levels at short treatment times (<8h). However, O-GlcNAc levels begins to recover at longer treatment times with OSMI-2[1]. A decrease in HCF-1 cleavage products and the appearance of uncleaved HCF-1 in cells treated with OSMI-2 (Compound 1b) is observed. Because OGT knockdown is known to decrease cell proliferation, the effects of OSMI-2 on cell growth in culture over 96h is also monitored. Although there is no evidence of apoptosis, the reduced growth of cells over time is observed, consistent with the knockdown results[1].
A time course performed with 20 μM OSMI-2 (Compound 1b) shows reciprocal changes in the abundance of OGT and OGA, with a particularly large increase in OGT; this may explain the recovery in O-GlcNAc levels with OSMI-2. At 24h where O-GlcNAc levels fully recovered[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 20 μM, 40 μM, 50 μM
Incubation Time: 4 hours, 24 hours
Result: Reduced O-GlcNAc levels.
Molecular Weight

555.62

Formula

C26H25N3O7S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC)CN(C([C@@H](C1=CC=CC=C1OC)NS(=O)(C2=CC3=C(NC(C=C3)=O)C=C2)=O)=O)CC4=CC=CS4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (179.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7998 mL 8.9990 mL 17.9979 mL
5 mM 0.3600 mL 1.7998 mL 3.5996 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.50 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (4.50 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7998 mL 8.9990 mL 17.9979 mL 44.9948 mL
5 mM 0.3600 mL 1.7998 mL 3.5996 mL 8.9990 mL
10 mM 0.1800 mL 0.8999 mL 1.7998 mL 4.4995 mL
15 mM 0.1200 mL 0.5999 mL 1.1999 mL 2.9997 mL
20 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2497 mL
25 mM 0.0720 mL 0.3600 mL 0.7199 mL 1.7998 mL
30 mM 0.0600 mL 0.3000 mL 0.5999 mL 1.4998 mL
40 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1249 mL
50 mM 0.0360 mL 0.1800 mL 0.3600 mL 0.8999 mL
60 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7499 mL
80 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
100 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4499 mL
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OSMI-2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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