Eeyarestatin-I-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEeyarestatinICat.No.:HY-110078CASNo.:412960-54-4分?式:C??H??Cl?N?O?分?量:630.44作?靶點(diǎn):p97;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(39.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.5862mL7.9310mL15.8619mL5mM0.3172mL1.5862mL3.1724mL10mM0.1586mL0.7931mL1.5862mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.25mg/mL(1.98mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性EeyarestatinI?種有效的內(nèi)質(zhì)?相關(guān)蛋?降解(ERAD)抑制劑，?種有效的蛋?易位抑制劑。EeyarestatinI靶向與p97相關(guān)的去泛素化過(guò)程(PAD)，并抑制依賴于atx3的去泛素化。EeyarestatinI通過(guò)促凋亡蛋?NOXA誘導(dǎo)細(xì)胞死亡，并具有抗癌作?。IC50&TargetEndoplasmicreticulum-associatedproteindegradation(ERAD)[1][2]體外研究EeyarestatinI(2.5-40μM;48hours;A549andH358cells)treatmentcausesadose-dependentcelldeathofbothA549andH358cells[1].EeyarestatinI(2.5-40μM;48hours;A549andH358cells)treatmentincreasesendoplasmicreticulum(ER)stressmarkersincludingBipandCHOPaslowas20μM.EeyarestatinItreatmentshowsadosedependentubiquitinationofkeyproteinsincludingPERKandIRE1α[1].EeyarestatinI(20μM;48hours;A549andH358cells)treatmentinducescellmigrationandcellinvasion[1].Eeyarestatin1preventsthetransferofnascentproteinsfromthemembrane-targetingcomplextotheERtranslocationmachinery,mostprobablybyinactivatingtheSec61complex[2].CellViabilityAssay[1]CellLine:A549andH358cellsConcentration:2.5μM,5μM,10μM,20μM,40μMIncubationTime:48hoursResult:CauseddosedependentcelldeathofbothA549andH358cells.WesternBlotAnalysis[1]CellLine:A549andH358cellsConcentration:2.5μM,5μM,10μM,20μM,40μMIncubationTime:48hoursResult:IncreasedERstressmarkersincludingBipandCHOP.REFERENCES[1].ParagPShah,etal.RegulationofVCP/p97demonstratesthecriticalbalancebetweencelldeathandepithelial-mesenchymaltransition(EMT)downstreamofERstress.Oncotarget.2015Jul10;6(19):17725-37.[2].BenedictCSCross,etal.EeyarestatinIinhibitsSec61-mediatedproteintranslocationattheendoplasmicreticulum.JCellSci.2009Dec1;122(Pt23):4393-400.[3].QiuyanWang,etal.Inhibitionofp97-dependentproteindegradationbyEeyarestatinI.JBiolChem.2008Mar21;283(12):7445-54.[4].QiuyanWang,etal.ERADinhibitorsintegrateERstresswithanepigeneticmechanismtoactivateBH3-onlyproteinNOXAincancercells.ProcNatlAcadSciUSA.2009Feb17;106(7):2200-5.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyva