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Nitrochin (4-NQO) is a chemical carcinogen. Nitrochin induces oncostatin-M (OSM) in esophageal cells. Nitrochin induces DNA damage, and induces apoptosis via a p53-dependent mitochondrial signaling pathway.

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CAS No. : 56-57-5

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Based on 3 publication(s) in Google Scholar

Other Forms of Nitrochin:

Top Publications Citing Use of Products

    Nitrochin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 26;44(1):220.  [Abstract]

    Nitrochin (4-NQO) (100 μg/mL; drinking water; 16 weeks). Representative images of the esophagus in Nitrochin (4NQO)-induced WT and Ttpal-KO mice.

    Nitrochin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 26;44(1):220.  [Abstract]

    Representative images of H&E-stained esophageal sections demonstrating morphological alterations, representative images of Ki-67 immunohistochemical and analysis revealing epithelial cell proliferation patterns. WT mice exhibited more advanced esophageal tumor stages than Ttpal-KO mice following Nitrochin (4-NQO) (100 μg/mL; drinking water; 16 weeks).

    Nitrochin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 26;44(1):220.  [Abstract]

    Nitrochin (4-NQO) (100 μg/mL; drinking water; 16 weeks). Tumor number and tumor size of esophagus in 4NQO-induced WT and Ttpal-KO mice.

    Nitrochin purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 Jul 16;23(1):519.  [Abstract]

    The ESCC mouse model was induced by feeding with Nitrochin (4-NQO) (drinking water; 100 μg/mL; 16 weeks). H&E-stained images of esophageal tissues from mice at 16, 30, and 32 weeks during the modeling period were obtained. By the 30th week, the esophageal epithelial structure became disordered, with cellular atypia, indicating the formation of intraepithelial neoplasia.

    Nitrochin purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 Jul 16;23(1):519.  [Abstract]

    Western blot analysis of fibrosis-related proteins in mouse tumor tissues. Expression of fibrosis-associated proteins in the ESCC group fed with Nitrochin (4-NQO) (drinking water; 100 μg/mL; 16 weeks) increased.

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    Description

    Nitrochin (4-NQO) is a chemical carcinogen. Nitrochin induces oncostatin-M (OSM) in esophageal cells. Nitrochin induces DNA damage, and induces apoptosis via a p53-dependent mitochondrial signaling pathway[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    CHO-AA8 IC50
    0.33 nM
    Compound: 4NQO
    Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
    Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
    [PMID: 2909741]
    In Vitro

    Nitrochin (4-NQO) (100 μg/mL; treated for 4 days) is used to treat normal human esophageal tissue. The results show that the number of senescent cells positive for oncostatin-M (OSM) in the treated tissue increases, the expression of OSM and its downstream target Stat3 significantly increases, while the expression of OSMR shows no change after treatment[1].
    Nitrochin (0.4-6 μM; 12-72 h) decreases the viability of KB cells in a time- and dose-dependent manner[1].
    Nitrochin (0.5-2.0 μM; treated for 12 hours) is used to treat KB cells. The results show that the apoptotic rate of cells gradually increases with the increase of Nitrochin dosage, and the cell viability decreases in a dose-dependent manner[2].
    Nitrochin (2.0 μM; 2-12 h) shows that the expression level of p53 in KB cells increases significantly. The expression of Bax gradually increases, while the expression of Bcl-2 continuously decreases. The activities of caspase-9 and caspase-3 are enhanced. The activity of caspase-3 reaches the maximum at 6 h and then decreases to some extent. DNA fragmentation starts at 6 h. The cell cycle is arrested in the G1 phase, and the expression level of p21Waf1/Cip1 gradually increases with the treatment time[2].

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

    Cell Viability Assay[2]

    Cell Line: KB cells
    Concentration: 0.4 μM, 0.6 μM, 1 μM, 2 μM, 4 μM, 6 μM
    Incubation Time: 12 h, 24 h, 48 h, 72 h
    Result: The viability of KB cells was decreased in a dose-dependent manner.

    Apoptosis Analysis[2]

    Cell Line: KB cells
    Concentration: 0.5 μM, 1.0 μM, 2.0 μM
    Incubation Time: 12 h
    Result: The apoptotic percentage of KB cells enhanced gradually along with the increase dosage.

    Cell Cycle Analysis[2]

    Cell Line: KB cells
    Concentration: 2 μM
    Incubation Time: 2 h, 8 h, 12 h
    Result: Induced cell cycle arrest of KB cells in G1 phase.

    RT-PCR[2]

    Cell Line: KB cells
    Concentration: 2 μM
    Incubation Time: 2 h, 8 h, 12 h
    Result: The expression level of p21Waf1/Cip1 was progressively increased.

    Western Blot Analysis[2]

    Cell Line: KB cells
    Concentration: 2 μM
    Incubation Time: 2 h, 8 h, 12 h
    Result: Increased the expression level of p53 and Bax, and decreased the expression level of Bcl-2.
    In Vivo

    Nitrochin (4-NQO) (100 μg/mL; administered via drinking water; continuously for 16 weeks) shows that senescent cells and oncostatin-M (OSM)-positive cells can be detected in the esophagus of mice, and esophageal cancer is induced in some mice[1].

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Nitrochin (200 μg/mL) induces oral squamous cell carcinoma (OSCC) in mice. An 8-week exposure yields tumors in 57% of mice by week 20, an effect boosted to 100% by Arecoline co-administration[3][4].A 20-week exposure drives universal and aggressive disease: tumors and lymph node enlargement emerge from week 25, with metastasis confirmed by weeks 28-36, culminating in 100% incidence of both primary and metastatic cancer by weeks 33-40[6].
    In Wistar rats, a 20-week oral exposure to Nitrochin (50 ppm) is required to induce invasive tongue squamous cell carcinoma, achieving a 70% success rate[5].
    Nitrochin (100 μg/mL) induces esophageal carcinogenesis in mice after a 16-week exposure[6][7][8].

    1.Induction of oral squamous cell carcinoma (OSCC)[3][4]
    Background
    Nitrochin induces DNA damage and triggers oxidative stress, which results in cell cycle dysregulation, evasion of apoptosis, and acquisition of unlimited proliferative potential, leading to the development of oral lesions[3][4].
    Specific Modeling Methods
    1.Mice: C57BL/6JNarl mice • male • 6-week-old
    Administration: Nitrochin (200 μg/mL) combined with Arecoline (500 μg/mL) • p.o. • dissolves in drinking water and can be consumed freely for 8 weeks
    2.Mice: C57BL/6JNarl mice • male • 6-week-old
    Administration: Nitrochin (200 μg/mL) • p.o. • dissolves in drinking water and can be consumed freely for 8 weeks;
    Modeling Indicators
    Molecular changes: Increased DNA damage markers
    Histology analysis: Lesions included squamous hyperplasia, dysplasia, and squamous cell carcinoma (SCC) (HE staining), Cytokeratin positive in tumor cells (Immunohistochemistry)

    Correlated Product(s): Arecoline (HY-N2364)
    2.Induction of tongue squamous cell carcinoma (TSCC)[5]
    Background
    Nitrochin induces DNA damage and triggers oxidative stress, which drives the development of tongue squamous cell carcinoma (TSCC)[5].
    Specific Modeling Methods
    Rats: Wistar rats • male bull; 8-week-old
    Administration: 50 ppm in drink water • p.o. • for 20 weeks;
    Modeling Indicators
    Histology analysis: squamous hyperplasia, dysplasia, and squamous cell carcinoma (SCC) (HE staining), ~70% incidence of dorsal invasive SCC
    3. Induction of esophageal squamous cell carcinoma (ESCC)[6][7][8]
    Background
    Nitrochin induces DNA damage and triggers oxidative stress, which drives the development of esophageal squamous cell carcinoma (ESCC)[6][7][8].
    Specific Modeling Methods
    1.Mice: C57BL/6J mice • female • 8-12-week-old
    Administration: 100 μg/mL • p.o. • dissolves in drinking water and can be consumed freely for 16 weeks; then maintained on control water for 12 weeks;
    2.Mice: C57BL/6J mice • female • 6-8-week-old
    Administration: 100 μg/mL • p.o. • dissolves in drinking water and can be consumed freely for 16 weeks; followed by drinking water containing 20% (v/v) ethanol for 12 weeks
    3.Mice: BALB/c mice • male • 6-week-old
    Administration: Nitrochin (200 μg/mL) • p.o. • dissolves in drinking water and can be consumed freely for 20 weeks
    Modeling Indicators
    Histology analysis: heterogeneous hyperplasia (NHA and rete pegs), papilloma, and invasive lesions

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

    Animal Model: C57BL/6J, p16+LUC, tdTOMp16+, K14E7Fancd2-/-, C57BL/6 Gfp+ mice[1]
    Dosage: 100 μg/mL; 10 μg/mL (for K14E7Fancd2-/- mice due to toxicity)
    Administration: Drinking water; continuously for 16 weeks
    Result: Luciferase positive senescent cells were detected in the esophagus, particularly at the gastrointestinal junction. And esophageal cancer was detected in the same regions where senescent cells were identified.
    Molecular Weight

    190.16

    Formula

    C9H6N2O3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=[N+](C1=C2C=CC=CC2=[N+]([O-])C=C1)[O-]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 40 mg/mL (210.35 mM; ultrasonic and warming and heat to 60°C; 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 5.2587 mL 26.2936 mL 52.5873 mL
    5 mM 1.0517 mL 5.2587 mL 10.5175 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (13.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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.
    In Vivo Dissolution Calculator
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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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

    Purity: 99.92%

    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 (protect from light). 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 5.2587 mL 26.2936 mL 52.5873 mL 131.4682 mL
    5 mM 1.0517 mL 5.2587 mL 10.5175 mL 26.2936 mL
    10 mM 0.5259 mL 2.6294 mL 5.2587 mL 13.1468 mL
    15 mM 0.3506 mL 1.7529 mL 3.5058 mL 8.7645 mL
    20 mM 0.2629 mL 1.3147 mL 2.6294 mL 6.5734 mL
    25 mM 0.2103 mL 1.0517 mL 2.1035 mL 5.2587 mL
    30 mM 0.1753 mL 0.8765 mL 1.7529 mL 4.3823 mL
    40 mM 0.1315 mL 0.6573 mL 1.3147 mL 3.2867 mL
    50 mM 0.1052 mL 0.5259 mL 1.0517 mL 2.6294 mL
    60 mM 0.0876 mL 0.4382 mL 0.8765 mL 2.1911 mL
    80 mM 0.0657 mL 0.3287 mL 0.6573 mL 1.6434 mL
    100 mM 0.0526 mL 0.2629 mL 0.5259 mL 1.3147 mL
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