1. Membrane Transporter/Ion Channel Immunology/Inflammation Anti-infection Apoptosis Stem Cell/Wnt
  2. Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Pyroptosis Wnt β-catenin
  3. Nigericin

Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC.

For research use only. We do not sell to patients.

Nigericin Chemical Structure

Nigericin Chemical Structure

CAS No. : 28380-24-7

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Customer Review

Based on 122 publication(s) in Google Scholar

Other Forms of Nigericin:

Top Publications Citing Use of Products

119 Publications Citing Use of MCE Nigericin

WB

    Nigericin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Mar 5;113:154743.  [Abstract]

    Priming with LPS (1 μg/mL; 4 h) and activating with Nigericin (10 μM; 2 h) induces NLRP3 expression, caspase-1 cleavage, and GSDMD cleavage in BMDMs.

    Nigericin purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2023 Mar 29.  [Abstract]

    Nigericin (1.38mM; 2 μg/2 μL; 10 min) signifcantly increases the expression of IL-1β, IL-18, and GSDMD N-terminal in rats

    Nigericin purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Jul;24(14):8078-8090.  [Abstract]

    LPS + Nigericin is used to induce pyroptosis as a positive control group.

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    • Biological Activity

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    • Customer Review

    Description

    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC[1][2][3][4][5][6][7].

    IC50 & Target

    NLRP3

     

    In Vitro

    Nigericin (0-4 μg/ml; 24 h) induces pyroptosis through caspase 1/GSDMD pathway in TNBC cells[6].
    Nigericin (1 μg/mL, 8 × MIC; 2 μg/mL, 16 × MIC; 196 h) is a bactericidal antibiotic against MDR gram-positive bacteria[4].
    Nigericin (0-0.25 μg/ml; 24 h) inactivates Wnt/β-catenin pathway in H460 cells as an anti-cancer effect[7].

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

    Cell Viability Assay[4]

    Cell Line: S. aureus, Staphylococcus epidermidis, Enterococcus faecalis, E. faecium, S. pneumoniae) , and Streptococcus agalactiae
    Concentration: 0 μg/ml, 0.05 μg/ml, 0.125 μg/ml, 0.25 μg/ml
    Incubation Time: 24 h
    Result: Exhibited potent activity against these clinical MDR strains, with MIC values ranging from 0.004-0.25 mg/ml.

    Western Blot Analysis[6]

    Cell Line: MDA-MB-231, and 4T1 cells
    Concentration: 0 μg/ml, 2 μg/ml, 4 μg/ml
    Incubation Time: 24 h
    Result: Showed increasing in the proteins level of caspase 1 and N-GSDMD.

    Cell Viability Assay[7]

    Cell Line: H460 cells
    Concentration: 0.5 μM, 1 μM, 2.5 μM
    Incubation Time: 24 h
    Result: Showed downregulating in the expression of proteins of the canonical Wnt (LRP6, Wnt5a/b, and β-catenin) signaling pathway.
    In Vivo

    Nigericin (1 mg/kg; i.p.; every 12 h for 3 D) reduces the infection of S. aureus USA300 in mice[4].
    Nigericin (0.025 mg/kg; s.c.; every two days in 4 weeks) plus anti-PD-1 shows synergistic anti-cancer effect[6].

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

    Animal Model: BALB/c Mice injected orthotopically with 4T1 cells[6]
    Dosage: 0.025 mg/kg
    Administration: Subcutaneous injection (s.c.)
    Result: Showed combination with anti-PD-1 antibody almost completely suppressed tumor growth.
    Animal Model: Mice Infected with S. aureus USA300[4]
    Dosage: 1 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Showed reduction in the bacterial burden to 1,000-10,000-fold in the major organs.
    Molecular Weight

    724.96

    Formula

    C40H68O11

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@H]1[C@](O[C@@H]2C[C@](CC[C@@H]3C)([H])O[C@@]3([H])[C@@H](C)C(O)=O)([C@@H]([C@H](OC)C2)C)O[C@](C)([C@]4([H])O[C@](C)([C@]5([H])O[C@]([C@@]([C@H](C[C@H]6C)C)([H])O[C@@]6(O)CO)([H])C[C@@H]5C)CC4)C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    Ethanol : ≥ 33.33 mg/mL (45.97 mM)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3794 mL 6.8969 mL 13.7939 mL
    5 mM 0.2759 mL 1.3794 mL 2.7588 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 (sealed storage, away from moisture). 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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    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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.45 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 EtOH 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% EtOH    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 EtOH 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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.37%

    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 (sealed storage, away from moisture). 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
    Ethanol 1 mM 1.3794 mL 6.8969 mL 13.7939 mL 34.4847 mL
    5 mM 0.2759 mL 1.3794 mL 2.7588 mL 6.8969 mL
    10 mM 0.1379 mL 0.6897 mL 1.3794 mL 3.4485 mL
    15 mM 0.0920 mL 0.4598 mL 0.9196 mL 2.2990 mL
    20 mM 0.0690 mL 0.3448 mL 0.6897 mL 1.7242 mL
    25 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3794 mL
    30 mM 0.0460 mL 0.2299 mL 0.4598 mL 1.1495 mL
    40 mM 0.0345 mL 0.1724 mL 0.3448 mL 0.8621 mL
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      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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