Importazole-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEImportazoleCat.No.:HY-101091CASNo.:662163-81-7分⼦式:C₂₀H₂₂N₄分⼦量:318.42作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥33mg/mL(103.64mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1405mL15.7025mL31.4051mL5mM0.6281mL3.1405mL6.2810mL10mM0.3141mL1.5703mL3.1405mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.85mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Importazole核转运受体importin-β的⼩分⼦抑制剂。体外研究Importazolespecificallyblocksimportin-β-mediatednuclearimportbothinXenopuseggextractsandculturedcells,withoutdisruptingtransportin-mediatednuclearimportorCRM1-mediatednuclearexport.Importazoleimpairsthereleaseofanimportin-βcargoFRETprobeandcausesbothpredictedandnoveldefectsinspindleassembly[1].ImportazoledisplaysanIC50ofapproximately15μMforinhibitionofNFAT-GFPimport.ImportazolehasanIC50ofapproximately22.5μMinHeLacellsfollowingtreatmentovera24-hourperiod[1].Importazoleinducesadose-andtime-dependentinhibitionofmyelomacellsgrowth.AndtheIC50valuesofimportazoleonRPMI8226andNCI-H929after48hoursincubationare(4.43±0.41)and(4.78±0.35)μmol/L,respectively.TreatmentofRPMI8226andNCI-H929cellswith8μmol/Limportazolefor24hcouldinhibitNF-κBimporttonucleusandreduceitsDNAbindingactivity[2].PROTOCOLCellAssay[1]HEK293cellsstablyexpressingNFAT-GFParegrownonglasscoverslipstoapproximately50%confluencypriortodrugtreatment.Inallcases,importazoleisusedat40μMandleptomycinBisusedat10ng/mL.Forcontrols,DMSOisusedataconcentrationof0.4%.Ionomycinisaddedat1.25μM.ImportazoleandleptomycinBtreatmentsareallfor1hour.Inallexperimentscellsarefixedwith4%formaldehydepriortofluorescencemicroscopy.DNAisvisualizedwith1μg/mLHoechstdye.Forquantification,100cellsfromeachconditionareanalyzedandthepercentagethatshowsnuclearaccumulationofNFAT-GFParecalculated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Nature.2018Nov;563(7729):131-136.•EMBORep.2019Jun;20(6):e47283.•JCellMolMed.2022Feb11.•OncoTargetsTher.2019Dec2;12:10455-10467.•PLoSOne.2020Nov12;15(11):e0242312.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].SoderholmJF,etal.Importazole,asmallmoleculeinhibitorofthetransportreceptorimportin-β.ACSChemBiol.2011Jul15;6(7):700-8.[2].YanWQ,etal.Effectofnuclearreceptorinhibitorimportazoleontheproliferationandapoptosisofmultiplemyelomacells.ZhonghuaXueYeXueZaZhi.2013Apr;34(4):323-6.McePdfHeightCaution:Producthasnotb