4E1RCat-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE4E1RCatCat.No.:HY-14427CASNo.:328998-25-0分⼦式:C₂₈H₁₈N₂O₆分⼦量:478.45作⽤靶点:EukaryoticInitiationFactor(eIF);Autophagy作⽤通路:CellCycle/DNADamage;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:18.33mg/mL(38.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0901mL10.4504mL20.9008mL5mM0.4180mL2.0901mL4.1802mL10mM0.2090mL1.0450mL2.0901mL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4E1RCat⼀种cap依赖性翻译抑制剂，能够抑制eIF4E:eIF4GI相互作⽤，IC50值约为4μM。IC50&TargeteIF4体外研究4E1RCatisaninhibitorofeIF4E:eIF4GIinteraction,withanIC50anof-4μM.4E1RCatbindingtoeIF4Ealso1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEinterfereswitheIF4Gand4E-BPbinding.4E1RCatinhibitsribosomerecruitmenttomRNAinacap-dependentmanner[1].4E1RCatblocksthecappedmRNAtranslation,andthetranslationisactivatedbyCDK1/CYCB1.Nearlyallnewproteinsynthesisinbothmitosisandinterphaseiscap-dependentand-sensitiveto4E1RCattreatment,inHeLaandU2OScells[2].体内研究4E1RCat(15mg/kg,i.p.)affactschemosensitivityofPten+/-Eμ-Myctumorsinmice.4E1RCat(15mg/kg,i.p.)sensitizesPten+/-Eμ-MycandTsc2+/-Eμ-Myclymphomastothecytotoxiceffectsofdoxorubicin(Dxr),and4E1RCattargetstranslationinmice[1].PROTOCOLCellAssay[1]TSC2+/-Eμ-MycandEμ-Myclymphomasareseededin96-wellplatesat106cells/mLinthepresenceofincreasingconcentrationsofdoxorubicin(Dxr)(rangingfrom3.9nMto250nM)and4E1RCat(rangingfrom78.13nMto10000nM)ataconstantratioofeither20:1or40:1.Twentyfourhourslater,aMTSassayisperformed.Tothisend,CellProliferationAssayisaddedtotheplatesandtheplatesfurtherincubatedforupto3h,followedbymeasuringtheOD490.ValuesobtainedarestandardizedagainstDMSOcontrols[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]OnemillionsecondaryPten+/-Eμ-Myc,Tsc2+/-Eμ-Myc,orEμ-Myclymphomacellsareinjectedintothetailveinof6-8weekoldfemaleC57BL/6mice.Whentumorsarepalpable,micearetreatedwithrapamycin(4mg/kgdailyfor5d),4E1RCat(15mg/kgdailyfor5d),ordoxorubicin(onceat10mg/kg).Compoundsareadministeredviaintraperitoneal(i.p.)injectionin5.2%PEG400/5.2%Tween80.Forcombinationstudies,rapamycinor4E1RCatareinjectedi.p.dailyforfiveconsecutivedays,withdoxorubicinbeingadministeredonceondaytwo.Animalsarepalpateddailytomonitorfortheonsetoftumors.Tumor-freesurvivalisdefinedasthetimebetweendisappearanceandreappearanceoftumors.Dataisanalyzedusingthelog-ranktestforstatisticalsignificancepresentedinKaplan-Meierformat[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•FrontOncol.2020Jun19;10:834.•JMolMed(Berl).2019Aug;97(8):1183-1193.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CencicR,etal.ReversingchemoresistancebysmallmoleculeinhibitionofthetranslationinitiationcomplexeIF4F.ProcNatlAcadSciUSA.2011Jan18;108(3):1046-51.[2].ShudaM,etal.CDK1substitutesformTORkinasetoactivatemitoticcap-dependentproteintranslation.ProcNatlAcadSciUSA.2015May12;112(19):5875-82.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Produc