Niclosamide-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemENiclosamideCat.No.:HY-B0497CASNo.:50-65-7分?式:C??H?Cl?N?O?分?量:327.12作?靶點(diǎn):STAT;Parasite;Antibiotic作?通路:JAK/STATSignaling;StemCell/Wnt;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMF:5mg/mL(15.28mM;Needultrasonic)掃描?維碼，DMSO:4.55mg/mL(13.91mM;Needultrasonic)運(yùn)?溶解?案計(jì)算器H2O:<0.1mg/mL(insoluble)獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0570mL15.2849mL30.5698mL5mM0.6114mL3.0570mL6.1140mL10mM0.3057mL1.5285mL3.0570mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請依序添加每種溶劑：10%DMF40%PEG3005%Tween-8045%salineSolubility:0.5mg/mL(1.53mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY1/4www.MedChemEwww.MedChemE?物活性Niclosamide(BAY2353)?種?服?物可利?的氯化?楊酰苯胺，具有驅(qū)?和潛在的抗腫瘤活性。Niclosamide(BAY2353)可抑制STAT3，在HeLa細(xì)胞中IC500.25μM，并在?細(xì)胞試驗(yàn)中抑制DNA復(fù)制。IC50&TargetSTAT30.25μM(IC50,inHeLacells)體外研究NiclosamideisaninhibitorofSTAT3,inhibitingSTAT3-mediatedluciferasereporteractivitywithanIC50of0.25μMinHeLacells.Niclosamide(1μM)inhibitstheEGF-inducednucleartranslocationofSTAT3inDu145cells.Niclosamide(<2μM)dosedependentlyinhibitsthetranscriptionofSTAT3downstreamgenesinDu145cells.Niclosamide(<10μM)inducesG0/G1arrestandapoptosisofDu145cancercellsinadosedependentmanner[1].NiclosamidecanblockSARS-CoVreplicationatamicromolarconcentrationinVeroE6cellsinfectedwithSARS-CoV[2].Niclosamide(<7.5μM)promotesFrizzled1endocytosis,downregulatesDishevelled-2protein,andinhibitsWnt3A-stimulatedbeta-cateninstabilizationandLEF/TCFreporteractivityinU2OScells[3].NiclosamideinhibitstheTNF-inducedNF-κBreporteractivityinadose-andtime-dependentmannerinU2OScells.Niclosamide(125nM)inhibitsNF-κBactivationinducedbyp65,IKKα,IKKβ,IKKγ,andTAK1inU2OScells.Niclosamide(<500nM)completelyblockthetime-anddose-dependentTNFα-inducedalterationoftheNF-κB-DNAcomplexinHL-60cells.Niclosamide(<10nM)inhibitsconstitutiveNF-κBactivationinU266cells.NiclosamideinhibitsTNF-induceddegradationofIκBαandrelocationofp65inadose-andtime-dependentmannerinHL-60,Molm13,orAMLprimarycells.Niclosamide(500nM)causesdecreaseinTNF-inducedNF-κB-dependentgeneproductsinvolvedincellsurvivalinHL-60cells.NiclosamidealsoinhibitsthegrowthandinducesrobustapoptosisofAMLcellsassociatedwithdecreasedMcl-1andXIAPlevelsandincreasedintracellularROSlevels[4].體內(nèi)研究Niclosamide(40mg/kg/d,i.p.)suppressesthegrowthofxenograftedAMLcellsinnudemicebearingHL-60xenografttumors[4].PROTOCOLKinaseAssay[1]AlloftheproteinkinasesareexpressedeitherinSf9insectcellsorinE.coliasrecombinantGST-fusionproteinsorHis-taggedproteins.Aradiometricproteinkinaseassayisusedformeasuringthekinaseactivityofthe22proteinkinases.Briefly,foreachproteinkinase,50μLreactioncocktailcontaining60mMHEPES-NaOH,3mMMgCl2,3mMMnCl2,3μMNa-orthovanadate,1.2mMDTT,50μg/mLPEG20000,1μM[γ-33P]-ATP,Niclosamide,adequateamountofenzymeanditssubstrate.ThePKC-alphaassayadditionallycontain1mMCa2,4mMEDTA,5μg/mLphosphatidylserineand1μg/mL1,2-Dioleyl-glycerol.Thereactioncocktailsareincubatedat37°Cfor60minutesandstopwith50μL2%(v/v)H3PO4.Incorporationof33Piisdeterminedwithamicroplatescintillationcounter.TheactivitiesandtheIC50valuesarecalculatedusingQuattroWorkflowV2.28.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Cellsareplatedin96-wellcultureplateswithcelldensityof3-4×103cells/wellandtreatwithNiclosamidebyadding100μLmediumcontainingNiclosamideofvariousconcentrationsonthesecondday.After72-hour'streatment,MTTisaddedtoeachwellandincubatedforadditional4-5hours,andtheabsorbanceismeasuredonamicroplatereaderat570nm.Cellgrowthinhibitionisevaluatedastheratiooftheabsorbanceofthesampletothatofthecontrol.Theresultsarerepresentativeofatleast3independent2/4www.MedChemEwww.MedChemEexperiments.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMalenu/nuBALB/cmiceareusedintheassay.HL-60cellsareinoculateds.c.ontheflanksof4-to6-wk-oldAdministration[4]mice.Tumorsaremeasuredeveryotherdaywithuseofcalipers.MicebearingHL-60xenograftsarerandomizedtoreceivetreatmentwithnormalsaline(control)orp-niclosamidefor15days(n=7animalseach).Tumorvolumesarecalculatedbythefollowingformula:a2×b×0.4,whereaisthesmallestdiameterandbisthediameterperpendiculartoa.Aftermiceareeuthanized,xenograftsaredissected,weighed,orpreserved.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellSyst.2018Apr25;6(4):424-443.e7.?BiochemPharmacol.2019Nov;169:113610.?Preprints.2021,2021040399.?Patent.US20180263995A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Ren,X.,etal.,Identificationofniclosamideasanewsmall-moleculeinhibitoroftheSTAT3signalingpathway.ACSMedicinalChemistryLetters,2010.1(9):p.454-459.[2].WuCJ,etal.Inhibitionofsevereacuterespiratorysyndromecoronavirusreplicationbyniclosamide.AntimicrobAgentsChemother.2004Jul;48(7):2693-6.[3].Chen,M.,etal.