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Nigericin sodium salt (Synonyms: NSC 292567)

Catalog No.GC15811

Nigericin sodium salt is an electrically neutral K +/H +?ionophore from Streptomyctus hygroscopicus an antibiotic that is lipophilic and selectively causes potassium to drain from the mitochondrial membrane.

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Nigericin sodium salt Chemical Structure

Cas No.: 28643-80-3

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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 6 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

H460 cells

Preparation Method

Migration and invasion assays were performed using cells serum-starved overnight. For migration assays, H-460 cells were seeded in Transwell inserts in RPMI 1640 with or without drugs or Nigericin sodium salt(1 uM). Inserts were placed in plates with RPMI 1640 containing 10% FBS in the presence of DMSO, or Nigericin sodium salt (1 uM). After 24 h, cell migration was quantified.

Reaction Conditions

1 µM Nigericin sodium salt for 24h

Applications

Nigericin sodium salt inhibited the migration and invasion of H460 lung cancer cells.

Animal experiment [2]:

Animal models

Nude mice(S18 cells were injected near the scapula of the nude mice)

Preparation Method

The mice were randomly divided into four groups with six animals each. DDP (2.5 mg/kg) was injected intraperitoneally for five continuous days and Nigericin sodium salt (4 mg/kg) was administrated intraperitoneally every two days.

Dosage form

4 mg/kg Nigericin sodium salt every two days.

Applications

Nigericin sodium salt significantly reduced tumor growth.

References:

[1]. Yakisich JS, Azad N, et,al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310. doi: 10.1177/1010428317694310. PMID: 28351327.

[2]. Deng CC, Liang Y, et,al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006. doi: 10.1016/j.biocel.2013.06.023. Epub 2013 Jul 4. PMID: 23831840.

Background

Nigericin sodium salt is an electrically neutral K +/H + ionophore from Streptomyctus hygroscopicus an antibiotic that is lipophilic and selectively causes potassium to drain from the mitochondrial membrane[8,9]. Nigericin sodium salt is a NLRP3 activator[1].

Nigericin sodium salt inhibited the migration and invasion of H460 lung cancer cells[1]. Nigericin sodium salt (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin sodium salt concentrations and a swelling effect at higher concentrations[2].Nigericin sodium salt exhibits higher toxicity on S18 cells than S26 cells, with IC50 of 2.03±0.55 μM and 4.77±2.35 μM, respectively. Nigericin sodium salt dramatically reduces the migration ability of S18 and HONE-1 cells[3]. Nigericin sodium salt exhibits toxicity for the HT29 and SW116 cell line with IC50 of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin sodium salt also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay[4].Using a combination of live-cell imaging and biochemical approaches, prototypical NLRP3 stimuli, the potassium ionophore nigericin, or millimolar concentrations of ATP exert both NLRP3-independent and -dependent effects on macrophages that result in cytokine release and cell death[5].Treatment of MN9D cells with Nigericin sodium salt led to an increase of LC3-II and p62 levels with concomitant activation of caspase. Ultrastructural examination revealed accumulation of autophagic vacuoles and swollen vacuoles in nigericin-treated cells[7].

In mice, Ngericin significantly reduces tumor growth. Nigericin sodium salt markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin sodium salt treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin sodium salt on CSCs in NPC[3].Nigericin sodium salt exerts anticancer effects on human osteosarcoma cancer cells by directly targeting STAT3. Nigericin sodium salt can significantly inhibit tumor migration and invasion. Nigericin sodium salt inhibits tumor growth in a mouse osteosarcoma model[6].

References:
[1]: Yakisich JS, Azad N, et,al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310. doi: 10.1177/1010428317694310. PMID: 28351327.
[2]: Bissinger R, Malik A, et,al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9. doi: 10.1111/bcpt.12503. Epub 2015 Nov 13. PMID: 26458067.
[3]: Deng CC, Liang Y, et,al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006. doi: 10.1016/j.biocel.2013.06.023. Epub 2013 Jul 4. PMID: 23831840.
[4]: Zhou HM, Dong TT, et,al. Suppression of colorectal cancer metastasis by nigericin through inhibition of epithelial-mesenchymal transition. World J Gastroenterol. 2012 Jun 7;18(21):2640-8. doi: 10.3748/wjg.v18.i21.2640. PMID: 22690072; PMCID: PMC3370000.
[5]: Heid ME, Keyel PA, et,al. Mitochondrial reactive oxygen species induces NLRP3-dependent lysosomal damage and inflammasome activation. J Immunol. 2013 Nov 15;191(10):5230-8. doi: 10.4049/jimmunol.1301490. Epub 2013 Oct 2. PMID: 24089192; PMCID: PMC3833073.
[6]: Yang Z, Xie J, et,al. Nigericin exerts anticancer effects through inhibition of the SRC/STAT3/BCL-2 in osteosarcoma. Biochem Pharmacol. 2022 Apr;198:114938. doi: 10.1016/j.bcp.2022.114938. Epub 2022 Jan 31. PMID: 35114189.
[7]: Lim J, Lee Y, et,al. Nigericin-induced impairment of autophagic flux in neuronal cells is inhibited by overexpression of Bak. J Biol Chem. 2012 Jul 6;287(28):23271-82. doi: 10.1074/jbc.M112.364281. Epub 2012 Apr 5. PMID: 22493436; PMCID: PMC3390606.
[8]: Fruth IA, Arrizabalaga G. Toxoplasma gondii: induction of egress by the potassium ionophore nigericin. Int J Parasitol. 2007 Dec;37(14):1559-67. doi: 10.1016/j.ijpara.2007.05.010. Epub 2007 Jun 9. PMID: 17618633; PMCID: PMC2221775.
[9]:Kucejova B, Kucej M, et,al. A screen for nigericin-resistant yeast mutants revealed genes controlling mitochondrial volume and mitochondrial cation homeostasis. Genetics. 2005 Oct;171(2):517-26. doi: 10.1534/genetics.105.046540. Epub 2005 Jul 14. PMID: 16020778; PMCID: PMC1456768.

Chemical Properties

Cas No. 28643-80-3 SDF
Synonyms NSC 292567
Formula C40H67NaO11 M.Wt 746.94
Solubility 25mg/mL in EtOH Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.3388 mL 6.694 mL 13.388 mL
5 mM 0.2678 mL 1.3388 mL 2.6776 mL
10 mM 0.1339 mL 0.6694 mL 1.3388 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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