OSMI-4

Catalog No.S8910 Batch:S891001

Technical Data

Formula

C₂₇H₂₆ClN₃O₇S₂

Molecular Weight

604.09

CAS No.

2260791-14-6

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (165.53 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5% DMSO 1 20% PEG300 2 3%Tween80 3 72%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 30 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 720 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells.

Targets

OGT ^[1]
(Cell-free assay)

3 μM(EC50)

Biological Activity

Description

OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells.

Targets

OGT ^[1]
(Cell-free assay)

3 μM(EC50)

In vitro

OSMI-4 reduces O-GlcNAc levels almost completely by 5 μM. A decrease in HCF-1 cleavage products and the appearance of uncleaved HCF-1 is observed in cells treated with OSMI-4. OSMI-4 is a kind of structure-based evolution of small molecule OGT inhibitors with low nanomolar binding affinities. OSMI-4 exhibits a ~3 μM EC50 in cells, making it especially attractive for probing OGT’s complex biology.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HEK293T cells Concentrations 5 μM, 10 μM, 20 μM Incubation Time 2 h, 8 h, 16 h, 24 h Method For quantitative analysis of the proteome, HEK293T cells in fresh media (changed 3 hours before treatment) are treated with 5 and 20 μM OSMI-4 in triplicates, and 10 μM in duplicates (11-plex) or DMSO for 8 hours, 16 hours or 24 hours. At the indicated time point, cells are lysed in lysis buffer (2 % SDS 50 mM Tris-HCl and 150 mM NaCl), sonicated and protein concentration determined with the BCA assay.

Cell Assay:^{^[1]}

Cell lines
HEK293T cells
Concentrations
5 μM, 10 μM, 20 μM
Incubation Time
2 h, 8 h, 16 h, 24 h
Method
For quantitative analysis of the proteome, HEK293T cells in fresh media (changed 3 hours before treatment) are treated with 5 and 20 μM OSMI-4 in triplicates, and 10 μM in duplicates (11-plex) or DMSO for 8 hours, 16 hours or 24 hours. At the indicated time point, cells are lysed in lysis buffer (2 % SDS 50 mM Tris-HCl and 150 mM NaCl), sonicated and protein concentration determined with the BCA assay.

References

[1] Sara E S Martin, et al. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545.

Selleck's OSMI-4 has been cited by 5 publications

Inhibition of DNMT1 methyltransferase activity via glucose-regulated O-GlcNAcylation alters the epigenome [ Elife, 2023, 12e85595]	PubMed: 37470704
FOXA1 O-GlcNAcylation-mediated transcriptional switch governs metastasis capacity in breast cancer [ Sci Adv, 2023, 9(33):eadg7112]	PubMed: 37595040
FOXA1 O-GlcNAcylation-mediated transcriptional switch governs metastasis capacity in breast cancer [ Sci Adv, 2023, 9(33):eadg7112]	PubMed: 37595040
O-GlcNAc transferase is important for homology-directed repair [ DNA Repair (Amst), 2022, 119:103394]	PubMed: 36095925
A 2D and 3D cell culture protocol to study O-GlcNAc in sphingosine-1-phosphate mediated fibroblast contraction [ STAR Protoc, 2022, 3(1):101113]	PubMed: 35118425

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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