4E2RCat-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE4E2RCatCat.No.:HY-100733CASNo.:432499-63-3分⼦式:C₂₂H₁₄ClNO₄S₂分⼦量:455.93作⽤靶点:EukaryoticInitiationFactor(eIF);Autophagy;VirusProtease作⽤通路:CellCycle/DNADamage;Autophagy;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:23.33mg/mL(51.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1933mL10.9666mL21.9332mL5mM0.4387mL2.1933mL4.3866mL10mM0.2193mL1.0967mL2.1933mL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%salineSolubility:2.33mg/mL(5.11mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性4E2RCateIF4E-eIF4G相互作⽤的抑制剂，IC50值为13.5μM。IC50&TargetIC50:13.5μM(eIF4E-eIF4G)[1]体外研究4E2RCatpreventstheinteractionbetweeneIF4E(thecap-bindingprotein)andeIF4G(alargescaffoldingprotein),inhibitingcap-dependenttranslation.Itsignificantlydecreaseshumancoronavirus229E(HCoV-229E)replication,reducingthepercentageofinfectedcellsandintra-andextracellularinfectiousvirustiters.4E2RCatinhibitscap-dependenttranslationinadose-dependentmanner.4E2RCatinhibitscap-dependentFFtranslationbutnotEMCVIRES-drivenRentranslation.4E2RCatinhibitscoronavirusreplicationinadose-andtime-dependentmanner[1].体内研究4E2RCatinhibitsproteinsynthesisinvivoanditisnotaconsequenceofincreasedcelldeath[1].PROTOCOLCellAssay[1]L132cellsaretreatedwith12.5μM4E2RCatfortheindicatedtimesandareprocessedforannexinV/propidiumiodidestaining.Tothisend,cellmediumiscollected.Cellsareishedwith1mLPBS,whichiscollectedaswell,andtrypsinizedin200μL0.05%trypsin-EDTA.Cellsarepooledwithpreviouslycollectedsupernatantsandspunfor2minat2,000rpmand4°C.Thecellpelletisishedwith2mLcoldPBS,followedbyanotherspin.Afterthesecondspin,thecellpelletisresuspendedin100μLannexinVbindingbufferandpropidiumiodideaddedtoafinalconcentrationof5μg/mL.Aftertheadditionof5μLannexinV-fluoresceinisothiocyanate,samplesareincubatedfor15mininthedarkatroomtemperatureanddiluted.Fluorescence-activatedcellsorter(FACS)analysesareperformedusingaFACScaninstrument[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Patent.US20220249439A1.•bioRxiv.May27,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CencicR,etal.BlockingeIF4E-eIF4Ginteractionasastrategytoimpaircoronavirusreplication.JVirol.2011Jul;85(13):6381-9.McePdfHeightCaution:Producthasnotbeenfullyvalidated