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Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemENigericin(sodiumsalt)(Standard)Cat.No.:HY-100381RCASNo.:28643-80-3分子式:C₄₀H₆₇NaO₁₁分子量:746.94作用靶点:PotassiumChannel;NOD-likeReceptor(NLR);Bacterial;Antibiotic;Pyroptosis;Wnt;β-catenin作用通路:MembraneTransporter/IonChannel;Immunology/Inflammation;Anti-infection;Apoptosis;StemCell/Wnt储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Nigericin(sodiumsalt)(Standard)是Nigericin(sodiumsalt)的分析标准品。本产品用于研究及分析应用。Nigericinsodiumsalt是一种抗生素(antibiotic),源自Streptomyceshygroscopicus,充当K+/H+离子载体(K+/H+ionophore),促进K+/H+跨线粒体膜交换。Nigericinsodiumsalt是NLRP3的激活剂。Nigericinsodiumsalt通过降低细胞内pH(pHi)和Wnt/β-catenin通路信号而显示出良好的抗癌活性。Nigericinsodiumsalt在TNBC中通过caspase1/GSDMD途径诱导细胞焦亡(pyroptosis)。体外研究Nigericin(0-4μg/mL;24h)sodiumsaltinducespyroptosisthroughcaspase1/GSDMDpathwayinTNBCcells[6].Nigericin(1μg/mL,8×MIC;2μg/mL,16×MIC;196h)sodiumsaltisabactericidalantibioticagainstMDRgram-positivebacteria[4].Nigericin(0-0.25μg/mL;24h)sodiumsaltinactivatesWnt/β-cateninpathwayinH460cellsasananti-cancereffect[7].CellViabilityAssay[4]CellLine:S.aureus,Staphylococcusepidermidis,Enterococcusfaecalis,E.faecium,S.pneumoniae),andStreptococcusagalactiaeConcentration:0μg/mL,0.05μg/mL,0.125μg/mL,0.25μg/mLIncubationTime:24h1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEResult:ExhibitedpotentactivityagainsttheseclinicalMDRstrains,withMICvaluesrangingfrom0.004-0.25mg/mL.WesternBlotAnalysis[6]CellLine:MDA-MB-231,and4T1cellsConcentration:0μg/mL,2μg/mL,4μg/mLIncubationTime:24hResult:Showedincreasingintheproteinslevelofcaspase1andN-GSDMD.体内研究Nigericin(1mg/kg;i.p.;every12hfor3D)sodiumsaltreducestheinfectionofS.aureusUSA300inmice[4].Nigericin(0.025mg/kg;s.c.;everytwodaysin4weeks)sodiumsaltplusanti-PD-1showssynergisticanti-cancereffect[6].AnimalModel:MiceInfectedwithS.aureusUSA300[4]Dosage:1mg/kgAdministration:Intraperitonealinjection(i.p.)Result:Showedreductioninthebacterialburdento1,000-10,000-foldinthemajororgans.AnimalModel:BALB/cMiceinjectedorthotopicallywith4T1cells[6]Dosage:0.025mg/kgAdministration:Subcutaneousinjection(s.c.)Result:Showedcombinationwithanti-PD-1antibodyalmostcompletelysuppressedtumorgrowth.REFERENCESZotovaL,etal.NovelcomponentsofanactivemitochondrialK(+)/H(+)exchange.JBiolChem.2010May7;285(19):14399-414.MariathasanS,etal.CryopyrinactivatestheinflammasomeinresponsetotoxinsandATP.Nature.2006Mar9;440(7081):228-32.BissingerR,etal.TriggeringofSuicidalErythrocyteDeathbytheAntibioticIonophoreNigericin.BasicClinPharmacolToxicol.2016May;118(5):381-9.XiaoliZhu,etal.Nigericiniseffectiveagainstmultidrugresistantgram-positivebacteria,persisters,andbiofilms.FrontCellInfectMicrobiol.2022Dec20:12:1055929.GuanzhuangGao,etal.Evidenceofnigericinasapotentialtherapeuticcandidateforcancers:Areview.BiomedPharmacother.2021May:137:111262.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemELishaWu,etal.NigericinBoostsAnti-TumorImmuneResponseviaInducingPyroptosisinTriple-NegativeBreastCancer.Cancers(Basel).2023Jun16;15(12):3221.JuanSebastianYakisich,etal.Nigericindecreasestheviabilityofmultidrug-resistantcancercellsandlungtumorspheresandpotentiatestheeffectsofcardiacglycosides.TumourBiol.2017Mar;39(3):1010428317694310.McePdfHeightCaution:Product

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