4EGI-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE4EGI-1Cat.No.:HY-19831CASNo.:315706-13-9分⼦式:C₁₈H₁₂Cl₂N₄O₄S分⼦量:451.28作⽤靶点:EukaryoticInitiationFactor(eIF);Autophagy;Apoptosis作⽤通路:CellCycle/DNADamage;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥35mg/mL(77.56mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2159mL11.0796mL22.1592mL5mM0.4432mL2.2159mL4.4318mL10mM0.2216mL1.1080mL2.2159mL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>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(5.54mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性4EGI-1⼀种eIF4E/eIF4G相互作⽤抑制剂，抑制eIF4E结合，Kd值为25μM。IC50&TargetKd:25μM(eIF4E/eIF4G)[1]体外研究4EGI-1isaninhibitorofeIF4E/eIF4Ginteraction,withaKdof25μMagainsteIF4Ebinding.4EGI-1disruptstheeIF4Fcomplexandinhibitsexpressionofoncogenicproteinsinmammaliancells.4EGI-1(0-40μM)alsoexhibitsproapoptoticactivityandinhibitsthegrowthofmultiplecancercelllines[1].4EGI-1iscytotoxictobreastcancercells,suchasSKBR-3,MCF-7andMDA-MB-231cells,withtheIC50ofappr30μM,andtothenon-CSCs(Cancerstemcells),theIC50isabout22μM.4EGI-1enhancesbreastCSCdifferentiation(40μM),andsuppressesbreastCSCinducedHUVECtube-likestructureformation(8μM).Moreover,4EGI-1selectivelyinhibitstranslationthatpersistsinCSCmaintenanceanddissemination[2].4EGI-1(50µM)impairstheformationofeIF4FcomplexinU87cells.4EGI-1(10,50and100µM)inhibitscellproliferationviainducingapoptosisinU87cells,andtheapoptosisisviaBaxactivation.4EGI-1causesmitochondrialdysfunction,andinducesERstressviaGRP-78activation,inU87cells[3].体内研究4EGI-1(75mg/kg,i.p.)inhibitsbreastcancerstemcells(CSC)tumorgrowthandtumorangiogenesisinvivo[2].4EGI-1(75mg/kg,i.p.)showsinhibitoryeffectonthetumorvolumeandweightinmicebearingU87cells[3].PROTOCOLCellAssay[2]1×104breastCSCsHMLER(CD44high/CD24low)FAcellsandotherindicatedbreastcancercellsaretreatedwithDMSO,or[E]-4EGI-1or[Z]-4EGI-1atseriesofconcentrationsfor24hours.Thecellsareperformedcellviabilityassayswithcellviabilityassaykit.Threeindependentexperimentsareperformed.AverageIC50resultsareshown(mean±SD,t-test,two-tailed)[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]Inthetumorxenograftedassay,1×105breastcancerstemcells(CSCs)aremixedwith100μLMatrigel/DMEMmixture(Matrigel:DMEM=1:2).BreastCSCs/Matrigel/DMEMmixturesareinjectedintoNOD/SCIDfemalemicemammaryglandsbysubcutaneousinjection.Afterthetumorformation(about75mm3involume,5mice/group),DMSO,or75mg/kg[E]-4EGI-1,or75mg/kg[Z]-4EGI-1isinjectedintothemicebyintraperitonealinjectiondailyfor30days.Tumorvolumesaremeasuredeverythreedays.Atthe30thday,micearesacrificedandtumorsareexcised.Tumorsweightsaremeasured.Tumortissuesamplesareusedforimmunohistostaining,Westernblotandimmunoprecipitationanalyses[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•NucleicAcidsRes.2022Jul18;gkac611.•NatCommun.2017Jun8;8:15617.•SciAdv.2022Jun24;8(25):eabo1782.•CellDeathDis.2020Nov15;11(11):982.•MolCancerTher.2018Dec;17(12):2676-2688.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MoerkeNJ,etal.Small-moleculeinhibitionoftheinteractionbetweenthetranslationinitiationfactorseIF4EandeIF4G.Cell.2007Jan26;128(2):257-67.[2].YiT,etal.4EGI-1targetsbreastcancerstemcellsbyselectiveinhibitionoftranslationthatpersistsinCSCmaintenance,proliferationandmetastasis.Oncotarget.2014Aug15;5(15):6028-37.[3].WuM,etal.Anti-CancerEffectofCap-TranslationInhibitor4EGI-1inHumanGliomaU87Cells:InvolvementofMitochondrialDysfunctionandERStress.CellPhysiolBiochem.2016;40(5):1013-1