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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Nigericin sodium salt) that retains the same biological activity.

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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Top Publications Citing Use of Products

96 Publications Citing Use of MCE Nigericin

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    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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    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.
    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

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    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

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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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