Art. -Nr.: HY-114361

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OSMI-4

28 Cited Publications

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Based on 28 publication(s) in Google Scholar

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC₅₀ of 3 μM in cells.

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Reinheit: 99.69%
CAS. Nr.: 2260791-14-6
Formel: C₂₇H₂₆ClN₃O₇S₂
Molecular Weight:604.09

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OSMI-4 Chemical Structure

CAS. Nr.: 2260791-14-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (28)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC₅₀ of 3 μM in cells.

IC₅₀ & Target

EC50: 3 μM (OGT)^[1].

Alle Acyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

OSMI-4 (4b) is the best OGT inhibitor reported to date, with a ～3 μM EC₅₀ in cells, making it especially attractive for probing OGT’s complex biology^[1].

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

Chemical Information

CAS. Nr. 2260791-14-6
Appearance Solid
Molecular Weight 604.09
Formel C₂₇H₂₆ClN₃O₇S₂
Color White to yellow
SMILES

O=C1C=CC2=C(C=C(Cl)C(S(N[C@@H](C(N(CC(OCC)=O)CC3=CC=CS3)=O)C4=C(OC)C=CC=C4)(=O)=O)=C2)N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (28)

All Cell Proliferation/Viability AssayWBCell Imaging/StainingFlow Cytometry

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Journal Impact Factor

Nat Commun

FBXO31-mediated ubiquitination of OGT maintains O-GlcNAcylation homeostasis to restrain endometrial malignancy. [Abstract]

2025 Feb 2;16(1):1274. PMID: 39894887

OSMI-4 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 2;16(1):1274. [Abstract]

OSMI-4 (20 µM; 72 h) significantly reduced the viability of endometrial cancer organoids (EC-Os) by inhibiting OGT.
J Biomed Sci

O-GlcNAc transferase couples MRE11 to transcriptionally active chromatin to suppress DNA damage. [Abstract]

2022 Feb 14;29(1):13. PMID: 35164752

OSMI-4 purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Feb 14;29(1):13. [Abstract]

C4-2 cell line was treated with 20 nM NVP2 or 20 nM NVP2 + 20 µM OSMI-4 for four hours, fractions isolated and samples analyzed using western blot. The results showed that OSMI‑4, an OGT inhibitor, antagonized the enhancement of MRE11 binding to chromatin caused by CDK9 inhibitor treatment.
Nat Cardiovasc Res

O-GlcNAcylation promotes angiogenic transdifferentiation to reverse vascular ischemia. [Abstract]

2025 Jul;4(7):904-920. PMID: 40615582

OSMI-4 purchased from MedChemExpress. Usage Cited in: Nat Cardiovasc Res. 2025 Jul;4(7):904-920. [Abstract]

Western blot analysis (left) and densitometry quantification (right) represent the expression levels of H3.3 in sorted YFP-positive and YFP-negative cells from vehicle and OSMI-4 (4 mg/kg; i.p.; once daily on days 0–2 post hindlimb ischemia surgery) treatment groups (n = 5 biologically independent replicates per group).

OSMI-4 purchased from MedChemExpress. Usage Cited in: Nat Cardiovasc Res. 2025 Jul;4(7):904-920. [Abstract]

Representative flow cytometry plots (left) and quantification (right) of YFP⁺ signal from the CD31⁺ population in mice treated with vehicle or OSMI-4 (4 mg/kg; i.p.; once daily on days 0–2 post hindlimb ischemia surgery) at day 7 after surgery. All flow cytometry plots are gated on live non-immune cells (DAPI^- CD11b^- or DAPI^- CD45^-, n = 3 mice per group; results are representative of two independent experiments).
Acta Biomater

Release of O-GlcNAc transferase inhibitor promotes neuronal differentiation of neural stem cells in 3D bioprinted supramolecular hydrogel scaffold for spinal cord injury repair. [Abstract]

2022 Oct 1:151:148-162. PMID: 36002129

OSMI-4 purchased from MedChemExpress. Usage Cited in: Acta Biomater. 2022 Oct 1:151:148-162. [Abstract]

Induction effect of OSMI-4 on neuronal differentiation of NSCs in vitro. Representative images of Tuj1⁺ (red, for neurons) and DAPI (blue, for nucleus) immunostaining of NSCs treated by OSMI-4 at varied concentrations. The results showed that the percentage of Tuj1-positive cells increased in a dose‑dependent manner with OSMI‑4 concentrations below 10 µM, but began to decrease at 10 µM.
Burns Trauma

Inhibiting Hyper-O-GlcNAcylation of c-Myc accelerate diabetic wound healing by alleviating keratinocyte dysfunction. [Abstract]

2021 Oct 8:9:tkab031. PMID: 34646892
Int J Biol Macromol

Buckwheat protein-derived peptide ameliorates insulin resistance by directing O-linked N-acetylglucosamine transferase to regulate the SIRT1/PGC1α pathway. [Abstract]

2025 Feb 11:140925. PMID: 39947565
Cell Rep

Paracrine stimulation of brown adipose tissue vascularization by adipocyte O-GlcNAc signaling. [Abstract]

2025 Dec 11;44(12):116678. PMID: 41385373
Cell Rep

O-GlcNAcylation of RBM14 contributes to elevated cellular O-GlcNAc through regulation of OGA protein stability. [Abstract]

2024 Apr 27;43(5):114163. PMID: 38678556
Cell Rep

Systematic analysis of the impact of phosphorylation and O-GlcNAcylation on protein subcellular localization. [Abstract]

2023 Jul 14;42(7):112796. PMID: 37453062
Neurosci Bull

OGT-Mediated O-GlcNAcylation of ATF2 Protects Against Sepsis-Associated Encephalopathy by Inhibiting Microglial Pyroptosis. [Abstract]

2025 May 24. PMID: 40411666
World J Diabetes

O-linked β-N-acetylglucosamine transferase regulates macrophage polarization in diabetic periodontitis: In vivo and in vitro study. [Abstract]

2025 Mar 15;16(3):95092. PMID: 40093279
iScience

O-GlcNAcylation regulates OTX2's proteostasis. [Abstract]

2023 Oct 12;26(11):108184. PMID: 38026167
J Biol Chem

Follicular cells protect Xenopus oocyte from abnormal maturation via integrin signaling downregulation and O-GlcNAcylation control. [Abstract]

2023 Aug;299(8):104950. PMID: 37354972
J Biol Chem

EGF promotes PKM2 O-GlcNAcylation by stimulating O-GlcNAc transferase phosphorylation at Y976 and their subsequent association. [Abstract]

2022 Sep;298(9):102340. PMID: 35931120
J Virol

Identification and characterization of O-GlcNAc modifications of a conserved orthopoxvirus core protein. [Abstract]

2025 May 23:e0005825. PMID: 40407344
RNA Biol

Inhibition of CDK9 activity compromises global splicing in prostate cancer cells. [Abstract]

2021 Nov 12;18(sup2):722-729. PMID: 34592899
Glycobiology

Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]

2024 Dec 10;34(12):cwae081. PMID: 39361894
Glycobiology

O-GlcNAc transferase maintains metabolic homeostasis in response to CDK9 inhibition. [Abstract]

2022 Aug 18;32(9):751-759. PMID: 35708495
J Cancer Res Clin Oncol

Castration-resistant prostate cancer cells are dependent on the high activity of CDK7. [Abstract]

2023 Jul;149(8):5255-5263. PMID: 36401094

OSMI-4 purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]

Depletion of OGT activity using OSMI-4 (20 µM; 0-96 h) signifcantly enhances the efcacy of CDK7 inhibitor YKL-5-124 (50 nM; 0-96 h) in three models of CRPC but not in the androgen-dependent LNCaP cell line or the normal prostate cells.

OSMI-4 purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]

OSMI-4 (20 µM; 4 days) and YKL-5-124 (1, 5, 10, 50, 400 nM; 4 days) demonstrate highly signifcant combinatorial toxicity on three CRPC models.
Exp Biol Med

PGM3 regulates beta-catenin activity to promote colorectal cancer cell progression. [Abstract]

2022 Sep;247(17):1518-1528. PMID: 35723049
Biochem Biophys Res Commun

Downregulation of O-GlcNAc transferase activity impairs basal autophagy and late endosome positioning under nutrient-rich conditions in human colon cells. [Abstract]

2024 Jun 3:724:150198. PMID: 38852504
bioRxiv

2025 Dec 11.
University of Konstanz

2025.
University of British Columbia

2025.
bioRxiv

2025 March 19.
Res Sq

2024 Jun 13.
SSRN

2023 Jun 15.
bioRxiv

Neuronal activity-driven O-GlcNAcylation promotes mitochondrial plasticity. [Abstract]

2023 Jan 11:2023.01.11.523512. PMID: 36711626

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (103.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6554 mL

8.2769 mL

16.5538 mL

5 mM

0.3311 mL

1.6554 mL

3.3108 mL

10 mM

0.1655 mL

0.8277 mL

1.6554 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Martin SES, et al. Structure-Based Evolution of Low Nanomolar O-GlcNAc Transferase Inhibitors. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6554 mL	8.2769 mL	16.5538 mL	41.3846 mL
	5 mM	0.3311 mL	1.6554 mL	3.3108 mL	8.2769 mL
	10 mM	0.1655 mL	0.8277 mL	1.6554 mL	4.1385 mL
	15 mM	0.1104 mL	0.5518 mL	1.1036 mL	2.7590 mL
	20 mM	0.0828 mL	0.4138 mL	0.8277 mL	2.0692 mL
	25 mM	0.0662 mL	0.3311 mL	0.6622 mL	1.6554 mL
	30 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3795 mL
	40 mM	0.0414 mL	0.2069 mL	0.4138 mL	1.0346 mL
	50 mM	0.0331 mL	0.1655 mL	0.3311 mL	0.8277 mL
	60 mM	0.0276 mL	0.1379 mL	0.2759 mL	0.6897 mL
	80 mM	0.0207 mL	0.1035 mL	0.2069 mL	0.5173 mL
	100 mM	0.0166 mL	0.0828 mL	0.1655 mL	0.4138 mL

Keywords

OSMI-4

28 Cited Publications

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OSMI-4

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) OSMI-4

Alle Acyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OSMI-4

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) OSMI-4

Alle Acyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OSMI-4 Related Classifications

Art. -Nr.: HY-114361