ER-000444793-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEER-000444793Cat.No.:HY-100852CASNo.:792957-74-5分⼦式:C₂₃H₁₈N₂O₂分⼦量:354.4作⽤靶点:MitochondrialMetabolism作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(141.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8217mL14.1084mL28.2167mL5mM0.5643mL2.8217mL5.6433mL10mM0.2822mL1.4108mL2.8217mL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。BIOLOGICALACTIVITY⽣物活性ER-000444793有效的线粒体通透性转换孔(mPTP)开放抑制剂。ER-000444793抑制mPTP，IC50为2.8μM。IC50&TargetIC50:2.8ꢀμM(mPTP)[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究ER-000444793isasmallmolecule,non-toxicmPTPinhibitorwithamechanismofactionindependentofCypDinhibition.ER-000444793potentlyanddose-dependentlyinhibitsCa2+-inducedmPT.ER-000444793bindsCypD,aCsA/CypDhomogenoustime-resolvedfluorescence(HTRF)assayisusedtostudycompoundbinding.BothCsAandSfAdose-dependentlydecreaseHTRFsignal,suggestingdisplacementoflabelledCsAfromrhCypDprotein(CsAIC50=23ꢀnMandSfAIC50=ꢀ5ꢀnM).Incontrast,ER-000444793hasnoeffectuptoaconcentrationof50ꢀμM,indicatinglackofdisplacementoflabelled-CsAfromrhCypDprotein.Together,thesedatasuggestthemechanismofER-000444793indelayingmPTisindependentofCypDfunctionalinhibition[1].PROTOCOLCellAssay[1]NFAT-RE-luc2Jurkatcellsarecollected,centrifugedat300ꢀgfor5ꢀminutesandre-suspendedinserum-freeRPMI-1640media,plussupplementswithoutantibiotic.Cellsuspension(15,000cells/20ꢀμL)isaddedtoeachwellofasolidblack384wellplateandincubatedinthepresenceofcompoundfor20ꢀhoursat37ꢀ°C.AlamarBlueisusedandisaddedtoeachwellat2xconcentrationinmediaandreactionallowedtoproceedfor4ꢀhoursat37ꢀ°C.Fluorescence(ex.540ꢀnm/em.590ꢀnm)isrecordedusingPherastarFS[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Biochemistry.2022Apr19;61(8):639-655.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BristonT,etal.IdentificationofER-000444793,aCyclophilinD-independentinhibitorofmitochondrialpermeabilitytransition,usingahigh-throughputscreenincryopreservedmitochondria.SciRep.2016Nov25;6:37798.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F