Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEImportazoleCat.No.:HY-101091CASNo.:662163-81-7分?式:C??H??N?分?量:318.42作?靶點:Apoptosis作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥33mg/mL(103.64mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1405mL15.7025mL31.4051mL5mM0.6281mL3.1405mL6.2810mL10mM0.3141mL1.5703mL3.1405mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.85mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性Importazole核轉運受體importin-β的?分?抑制劑。體外研究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.戶使?本產品發表的科研?獻?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?邊的抑制劑?師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