Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes[1].Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner[2]. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis[3].
IC50 & Target
K+/H+ ionophore[1]
分子量
724.96
Formula
C40H68O11
CAS 号
28380-24-7
中文名称
尼日利亚霉素
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zotova L, et al. Novel components of an active mitochondrial K(+)/H(+) exchange. J Biol Chem. 2010 May 7;285(19):14399-414.
[2]. Mariathasan S, et al.Cryopyrin activates the inflammasome in response to toxins and ATP.Nature. 2006 Mar 9;440(7081):228-32.
[3]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9.
Nigericin sodium salt 是从吸水链霉菌中得到的一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用,NLRP3 的激动剂。
Nigericin sodium salt Chemical Structure
CAS No. : 28643-80-3
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价格
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数量
5 mg
¥900
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10 mg
¥1500
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100 mg
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生物活性
Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore, a NLRP3 activator[1].
体外研究 (In Vitro)
Nigericin (0.1 µM) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a dose dependent manner. Nigericin inhibits migration and invasion of H460 lung cancer cells[1]. Nigericin (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higher concentrations. Nigericin (0.1-1 nM) significantly decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and 10 nM[2]. Nigericin 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 can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces the migration ability of S18 and HONE-1 cells[3]. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC50 of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Ngericin (4 mg/kg, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agent DDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin on CSCs in NPC[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
746.94
Formula
C40H67NaO11
CAS 号
28643-80-3
中文名称
尼日利亚菌素钠盐;尼日利亚菌素钠
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Yakisich JS, 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
[2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9
[3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006
[4]. Zhou HM, 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
Cell Assay [1]
For RCCs, cells (appr 2000 cells/well) are plated in 96-well cell-culture microplates and incubated over nigericinht in complete media (CM)-RPMI 1640 supplemented with 5% FBS and 2 mM l-glutamine. Cells are then exposed to the appropriate concentration of drug or vehicle for 72 h. For PPSS, cells (appr 500 cells/well) are plated in 96-well cell-culture microplates incubated over Nigericinht in CM to allow them to adhere and then maintained in serum-free media for 7-8 days and then treated with the appropriate concentration of drug or vehicle for 72 h in SFM. Cell viability for cells growing under RCCs and PPSS are evaluated by the MTT assay. The absorbance of solubilized formazan is read at 570 nm using ELISA (enzyme-linked immunosorbent assay) reader. In all cases, the highest concentration of DMSO is used in the control and this concentration is maintained below 0.001% (v/v). This DMSO concentration does not show any significant antiproliferative effect on the cell line in a short-term assay.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [3]
Mice[3] The S18 cells are injected near the scapula of the nude mice. Nine days after injection, the mice are randomly divided into four groups with six animals each (control, DDP, Nigericin and DDP combined with Nigericin). DDP (2.5 mg/kg) is injected intraperitoneally for five continuous days and nigericin (4 mg/kg) is administrated intraperitoneally every two days. Tumor length and width are measured with a vernier caliper every other day. Tumor volume is calculated using the formula V=0.5×(length×width2). The body weights of the mice are recorded every two days. Mice are humanely euthanized when the tumor volume reach 2000 mm3.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Yakisich JS, 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
[2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9
[3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006
[4]. Zhou HM, 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