Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE4E1RCatCat.No.:HY-14427CASNo.:328998-25-0分?式:C??H??N?O?分?量:478.45作?靶點:EukaryoticInitiationFactor(eIF);Autophagy作?通路:CellCycle/DNADamage;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:18.33mg/mL(38.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0901mL10.4504mL20.9008mL5mM0.4180mL2.0901mL4.1802mL10mM0.2090mL1.0450mL2.0901mL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?。BIOLOGICALACTIVITY?物活性4E1RCat?種cap依賴性翻譯抑制劑，能夠抑制eIF4E:eIF4GI相互作?，IC50值約為4μM。IC50&TargeteIF4體外研究4E1RCatisaninhibitorofeIF4E:eIF4GIinteraction,withanIC50anof-4μM.4E1RCatbindingtoeIF4Ealso1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEinterfereswitheIF4Gand4E-BPbinding.4E1RCatinhibitsribosomerecruitmenttomRNAinacap-dependentmanner[1].4E1RCatblocksthecappedmRNAtranslation,andthetranslationisactivatedbyCDK1/CYCB1.Nearlyallnewproteinsynthesisinbothmitosisandinterphaseiscap-dependentand-sensitiveto4E1RCattreatment,inHeLaandU2OScells[2].體內研究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.戶使?本產品發表的科研?獻?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?邊的抑制劑?師www.MedChemECaution:Produc