Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE4E2RCatCat.No.:HY-100733CASNo.:432499-63-3分?式:C??H??ClNO?S?分?量:455.93作?靶點:EukaryoticInitiationFactor(eIF);Autophagy;VirusProtease作?通路:CellCycle/DNADamage;Autophagy;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:23.33mg/mL(51.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1933mL10.9666mL21.9332mL5mM0.4387mL2.1933mL4.3866mL10mM0.2193mL1.0967mL2.1933mL請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)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%salineSolubility:2.33mg/mL(5.11mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性4E2RCateIF4E-eIF4G相互作?的抑制劑，IC50值為13.5μM。IC50&TargetIC50:13.5μM(eIF4E-eIF4G)[1]體外研究4E2RCatpreventstheinteractionbetweeneIF4E(thecap-bindingprotein)andeIF4G(alargescaffoldingprotein),inhibitingcap-dependenttranslation.Itsignificantlydecreaseshumancoronavirus229E(HCoV-229E)replication,reducingthepercentageofinfectedcellsandintra-andextracellularinfectiousvirustiters.4E2RCatinhibitscap-dependenttranslationinadose-dependentmanner.4E2RCatinhibitscap-dependentFFtranslationbutnotEMCVIRES-drivenRentranslation.4E2RCatinhibitscoronavirusreplicationinadose-andtime-dependentmanner[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?Patent.US20220249439A1.?bioRxiv.May27,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CencicR,etal.BlockingeIF4E-eIF4Ginteractionasastrategytoimpaircoronavirusreplication.JVirol.2011Jul;85(13):6381-9.McePdfHeightCaution:Producthasnotbeenfullyvalidated