Zileuton
Based on 20 publication(s) in Google Scholar
Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 111406-87-2
- Formula: C11H12N2O2S
- Molecular Weight:236.30
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Zileuton
More- Nat Commun. 2024 Sep 10;15(1):7914. [Abstract]
- Redox Biol. 2024 May:71:103096. [Abstract]
- J Neuroinflammation. 2025 Aug 28;22(1):208. [Abstract]
- Cell Death Dis. 2025 May 19;16(1):403. [Abstract]
- J Cachexia Sarcopenia Muscle. 2022 Aug;13(4):2242-2253. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Emerg Microbes Infect. 2022 Dec;11(1):1806-1818. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Ethnopharmacol. 2023 Jun 12:309:116357. [Abstract]
- Int J Mol Sci. 2022 Apr 28;23(9):4910. [Abstract]
- Front Cell Infect Microbiol. 2022 Feb 4;12:825824. [Abstract]
- J Cell Mol Med. 2025 Jun;29(11):e70641. [Abstract]
- Proteomics. 2018 Aug;18(15):e1700388. [Abstract]
- Head Neck. 2025 Feb;47(2):504-516. [Abstract]
- Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. [Abstract]
- Northwestern University. 2026.
- University of Padua. 2024.
- bioRxiv. 2024 Jul 7:2024.07.04.601620. [Abstract]
- Oxid Med Cell Longev. 2022 Feb 9;2022:4295208. [Abstract]
- Oxid Med Cell Longev. 2019 Nov 3;2019:7536803. [Abstract]
Customer Validation & Images
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IF
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WB
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Cell Proliferation/Viability Assay
Biological Activity
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5-LOX |
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Cell Line
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Type | Value | Description | References |
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| BMMC | IC50 |
>20 μM
Compound: zileuton
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Antiosteoclast activity in mouse BMM cells assessed as reduction of RANKL-induced osteoclasts differentiation by measuring TRAP positive multinucleated cells after 4 days by light microscopy
Antiosteoclast activity in mouse BMM cells assessed as reduction of RANKL-induced osteoclasts differentiation by measuring TRAP positive multinucleated cells after 4 days by light microscopy
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[PMID: 26432605] |
| HeLa | IC50 |
0.04 μg/mL
Compound: Zileuton
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Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
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[PMID: 19942440] |
| MC9 | IC50 |
0.55 μM
Compound: zileuton
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Inhibition of LTB4 production in mouse MC9 cells
Inhibition of LTB4 production in mouse MC9 cells
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[PMID: 18498150] |
| PMNL | IC50 |
0.5 μM
Compound: zileuton
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Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis
Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis
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[PMID: 22551629] |
| RBL-1 | IC50 |
0.5 μM
Compound: A-64077
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The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1
The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1
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[PMID: 1635053] |
| RBL-1 | IC50 |
100 nM
Compound: 1, (A-64077)
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Compound was tested for in vitro inhibition on broken RBL-1.
Compound was tested for in vitro inhibition on broken RBL-1.
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[PMID: 8709092] |
| RBL-1 | IC50 |
3.2 μM
Compound: zileuton
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Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells
Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells
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[PMID: 8831759] |
| RBL-1 | IC50 |
0.5 μM
Compound: 1a
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Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production
Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production
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[PMID: 9207936] |
| RBL-1 | IC50 |
0.14 μM
Compound: A-64077 (Zileuton, 5)
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Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells
Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells
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10.1016/S0960-894X(00)80622-8 |
| RBL-2H3 | IC50 |
804 nM
Compound: zileuton
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Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells
Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells
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[PMID: 9599246] |
| RBL-2H3 | IC50 |
1.25 μM
Compound: Zileuton
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In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells.
In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells.
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10.1016/0960-894X(95)00088-B |
| Sf21 | IC50 |
564.4 μM
Compound: Zileuton
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Zileuton
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 111406-87-2
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Appearance Solid
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Molecular Weight 236.30
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Formula C11H12N2O2S
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Color White to off-white
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SMILES
CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1
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Synonyms
A 64077; Abbott 64077
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (20)
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Journal Impact Factor
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Most Recent
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Nat Commun
A mouse protozoan boosts antigen-specific mucosal IgA responses in a specific lipid metabolism- and signaling-dependent manner. [Abstract]2024 Sep 10;15(1):7914. PMID: 39256385 -
Redox Biol
Excessive linoleic acid induces muscle oxidative stress through 5-lipoxygenase-dependent peroxidation. [Abstract]2024 May:71:103096. PMID: 38387137 -
J Neuroinflammation
P2X7-CaMKII drives 5-LOX nuclear translocation to impair microglial function after subarachnoid hemorrhage. [Abstract]2025 Aug 28;22(1):208. PMID: 40877894 -
Cell Death Dis
A novel taxane SB-T-101141 triggers a noncanonical ferroptosis to overcome Paclitaxel resistance of breast cancer via iron homeostasis-related KHSRP. [Abstract]2025 May 19;16(1):403. PMID: 40389408 -
J Cachexia Sarcopenia Muscle
A disease-associated missense mutation in CYP4F3 affects the metabolism of leukotriene B4 via disruption of electron transfer. [Abstract]2022 Aug;13(4):2242-2253. PMID: 35686338 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Emerg Microbes Infect
Gut dysbacteriosis attenuates resistance to Mycobacterium bovis infection by decreasing cyclooxygenase 2 to inhibit endoplasmic reticulum stress. [Abstract]2022 Dec;11(1):1806-1818. PMID: 35766265 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
J Ethnopharmacol
Involvement of p38 MAPK/cPLA2 and arachidonic acid metabolic pathway in Shengmai injection-induced pseudo-allergic reactions. [Abstract]2023 Jun 12:309:116357. PMID: 36906156 -
Int J Mol Sci
Zileuton, a 5-Lipoxygenase Inhibitor, Attenuates Haemolysate-Induced BV-2 Cell Activation by Suppressing the MyD88/NF-κB Pathway. [Abstract]2022 Apr 28;23(9):4910. PMID: 35563304 -
Front Cell Infect Microbiol
Dysregulation of Cytosolic c-di-GMP in Edwardsiella piscicida Promotes Cellular Non-Canonical Ferroptosis. [Abstract]2022 Feb 4;12:825824. PMID: 35186798 -
J Cell Mol Med
Downregulation of Alox5 Inhibits Ferroptosis to Improve Doxorubicin-Induced Cardiotoxicity via the P53/SLC7A11 Pathway. [Abstract]2025 Jun;29(11):e70641. PMID: 40485049 -
Proteomics
Integrative Analysis of Proteome and Ubiquitylome Reveals Unique Features of Lysosomal and Endocytic Pathways in Gefitinib-Resistant Non-Small Cell Lung Cancer Cells. [Abstract]2018 Aug;18(15):e1700388. PMID: 29901268
Zileuton purchased from MedChemExpress. Usage Cited in: Proteomics. 2018 Aug;18(15):e1700388. [Abstract]
Comparison of Gefitinib resistant colony formation between PC9/GR cells treated with the control (DMSO) or 200uM Zileuton.
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Head Neck
2025 Feb;47(2):504-516. PMID: 39290130 -
Biochem Biophys Res Commun
Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]2018 Sep 3;503(1):297-303. PMID: 29890135 -
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bioRxiv
Rebalancing Viral and Immune Damage versus Tissue Repair Prevents Death from Lethal Influenza Infection. [Abstract]2024 Jul 7:2024.07.04.601620. PMID: 39372755 -
Oxid Med Cell Longev
Cepharanthine Attenuates Early Brain Injury after Subarachnoid Hemorrhage in Mice via Inhibiting 15-Lipoxygenase-1-Mediated Microglia and Endothelial Cell Ferroptosis. [Abstract]2022 Feb 9;2022:4295208. PMID: 35186185 -
Oxid Med Cell Longev
The 5-Lipoxygenase Inhibitor Zileuton Protects Pressure Overload-Induced Cardiac Remodeling via Activating PPAR α. [Abstract]2019 Nov 3;2019:7536803. PMID: 31781348
Zileuton purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803. [Abstract]
Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).
Zileuton purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803. [Abstract]
Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).
Solvent & Solubility
DMSO : 100 mg/mL (423.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 10 mg/mL (42.32 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 10 mg/mL (42.32 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (21.16 mM); Clear solution; Need ultrasonic
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
Rats: Rats are randomized into 6 groups (n=12 per group): sham I/R group, I/R group, zileuton+I/R group, zileuton+indomethacin+I/R group, zileuton+ketorolac+I/R group, and zileuton+nimesulide+I/R group. 5-LOX inhibitor zileuton (5 mg/kg, orally twice daily) is given alone or with non-selective COX inhibitor indomethacin (5 mg/kg, intraperitoneally), selective COX-1 inhibitor ketorolac (10 mg/kg, orally) or selective COX-2 inhibitor nimesulide (10 mg/kg, subcutaneously). COX inhibitors are given 15 minutes before zileuton administration. All drugs are given for 3 days prior to I/R or sham I/R procedure. Dose of zileuton (5 mg/kg, twice daily) is used in this study. Rats in sham I/R group receive the vehicle of zileuton orally. Zileuton is dissolved in dimethyl sulfoxide (DMSO) and further dilutions are made using saline to achieve a final DMSO concentration of 1%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10 [Content Brief]
[2]. Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner [Content Brief]
[3]. Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402 [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2319 mL | 21.1595 mL | 42.3191 mL | 105.7977 mL |
| 5 mM | 0.8464 mL | 4.2319 mL | 8.4638 mL | 21.1595 mL | |
| 10 mM | 0.4232 mL | 2.1160 mL | 4.2319 mL | 10.5798 mL | |
| 15 mM | 0.2821 mL | 1.4106 mL | 2.8213 mL | 7.0532 mL | |
| 20 mM | 0.2116 mL | 1.0580 mL | 2.1160 mL | 5.2899 mL | |
| 25 mM | 0.1693 mL | 0.8464 mL | 1.6928 mL | 4.2319 mL | |
| 30 mM | 0.1411 mL | 0.7053 mL | 1.4106 mL | 3.5266 mL | |
| 40 mM | 0.1058 mL | 0.5290 mL | 1.0580 mL | 2.6449 mL | |
| 50 mM | 0.0846 mL | 0.4232 mL | 0.8464 mL | 2.1160 mL | |
| 60 mM | 0.0705 mL | 0.3527 mL | 0.7053 mL | 1.7633 mL | |
| 80 mM | 0.0529 mL | 0.2645 mL | 0.5290 mL | 1.3225 mL | |
| 100 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0580 mL |
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