ML385-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML385Cat.No.:HY-100523CASNo.:846557-71-9分⼦式:C₂₉H₂₅N₃O₄S分⼦量:511.59作⽤靶点:Keap1-Nrf2;Ferroptosis作⽤通路:NF-κB;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(65.15mM;ultrasonicandwarmingandheatto60°C)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9547mL9.7735mL19.5469mL5mM0.3909mL1.9547mL3.9094mL10mM0.1955mL0.9773mL1.9547mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.07mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.89mM);Clearsolution3.请依序添加每种溶剂：15%SolutolHS15>>10%CremophorEL>>35%PEG400>>40%waterSolubility:5mg/mL(9.77mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:10mg/mL(19.55mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性ML385特异的NRF2抑制剂，IC50为1.9μM。IC50&TargetIC50:1.9μM(NRF2)[1]体外研究ML385interactswithNRF2andaffectstheDNAbindingactivityoftheNRF2-MAFGproteincomplex.TheadditionofML385decreasesanisotropyinadose-dependentmanner,withanIC50of1.9μM.Adose-dependentreductionintheNRF2transcriptionalactivityisobservedandthemaximuminhibitoryconcentrationis5μMbyML385.TreatmentwithML385leadstoasignificantreductioninNRF2anddownstreamtargetgeneexpressionselectivelyinKEAP1mutantH460cells.ML385selectivelyaffectsthecolonyformingabilityorgrowthoflungcancercellswithgainofNRF2function[1].体内研究ML385incombinationwithcarboplatinleadstoasignificantreductionintumorcellproliferation,demonstratedbyfewerKi-67positivecells.TumorsamplestreatedwithML385showasignificantreductioninNRF2proteinlevelanditsdownstreamtargetgenes[1].ML385(intraperitonealinjection;30mg/kg;7days)weakensthetherapeuticeffectsofMSC-Exooninflammation-inducedastrocyticactivationinmice,andreducesreactiveastrogliosis,NF-κBdeactivation[3].AnimalModel:8-week-oldC57B/6malemice[3]Dosage:30mg/kg;7daysAdministration:IntraperitonealinjectionResult:ReversedinhibitionofMSC-Exoonhippocampalastrocyticactivationinvivo.户使⽤本产品发表的科研⽂献•Nature.2022Oct;610(7931):366-372.•CancerCell.2021May10;39(5):678-693.e11.•NatCommun.2018Oct24;9(1):4429.•Biomaterials.2020Oct;257:120264.•ActaPharmSinB.2021May;11(5):1246-1260.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].SinghA,etal.SmallMoleculeInhibitorofNRF2SelectivelyIntervenesTherapeuticResistanceinKEAP1-DeficientNSCLCTumors.ACSChemBiol.2016Nov18;11(11):3214-3225.[2].XinnongLiu,etal.IsoliquiritigeninamelioratesacutepancreatitisinmiceviainhibitionofoxidativestressandmodulationoftheNrf2/HO-1pathway.OxidMedCellLongev.20March2018.[3].XianP,etal.Mesenchymalstemcell-derivedexosomesasananotherapeuticagentforameliorationofinflammation-inducedastrocytealterationsinmice.Theranostics.2019Aug14;9(20):5956-5975.McePdfHeightCaution:Product