ML327-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML327Cat.No.:HY-103038CASNo.:1883510-31-3分⼦式:C₁₉H₁₈N₄O₄分⼦量:366.37作⽤靶点:c-Myc;Autophagy作⽤通路:Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:32mg/mL(87.34mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7295mL13.6474mL27.2948mL5mM0.5459mL2.7295mL5.4590mL10mM0.2729mL1.3647mL2.7295mL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。BIOLOGICALACTIVITY⽣物活性ML327MYC的阻断剂，也可以去阻遏E-钙粘蛋⽩转录和逆转上⽪-间质转化(EMT)。IC50&TargetMYC[1]体外研究TreatmentwithML327inducesanelongatedmorphologyinneuroblastomacells.BE(2)-Ccellstreatedwith1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEML327demonstratesG1cellcyclearrestwithaconcordantdecreaseinSphasepopulation,andasignificantincreaseinthesubG0population.ML327inducestheexpressionofCDH1inallsevenoftheneuroblastomacelllineswitha50to1,400-foldinductionofCDH1mRNAexpression.ML327blockstheexpressionofMYCfamilyofoncogenictranscriptionfactorsinalltestedneuroblastomacelllines.ImmunoblottingtimecoursedemonstratesearlyrepressionofN-MYCexpressionwithin2hoftreatmentwithML327(10µM).p53levelsarealsosuppressedbytreatmentwithML327.ML327-pretreatedcellsdemonstratesreducedproliferativepotentialinbothtetrazolium-based(p[1].ML327reducesSW620invcellinvasionthroughMatrigelby~60%andreducesH520cellinvasionby~30%intheseinvitroassays.ML327partiallyrestoresE-cadherinexpressionattheplasmamembraneinNMuMGcellsinducedtoundergoEpithelial-to-MesenchymalTransition(EMT)byTGF-β1treatment[2].体内研究ML327treatmentsignificantlyreducestumorvolumebythree-foldoverthetwo-weektreatmentperiod(p=0.02).Tumorexplantweightsareapproximatelythree-foldsmallerintheML327-treatedmice(p=0.01).MicetreatedwithML327lost12%morebodyweightthanvehicletreatedmice.ML327treatmentresultsinatwo-folddecreaseinMYCNexpression,confirmingthatML327inhibitsxenograftMYCNexpression(p=0.0035)[1].PROTOCOLCellAssay[1]Cellsareseededonto96-wellplatesatequivalentdensity(3,000to10,000dependinguponcellline),permittedtoattachovernight,andtreatedwitheitherML327(10μM)orvehicle.Dailyabsorbancemeasurements(450nm)usingthecellcountingkitareobtained.ForestimationofIC50values,cellsareplatedatequaldensity,permittedtoattach,andbaselineabsorbanceisobtainedusingcellcountingkit.CellsarethentreatedwithvaryingdosesofML327(0.1to30μM)andcellviabilityismeasured72haftertreatment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleathymicnudemice(4to6weeksold)aremaintainedasdescribed.BE(2)-CcellsxenograftsareAdministration[1]establishedaspreviouslydescribed.Briefly,1×106cells/100µLofHBSSareinjectedsubcutaneouslyintoflanksusinga26-gaugeneedle(n=10pergroup).Micearemonitoreddailyforxenograftformationandassessedbymeasuringthetwogreatestperpendiculartumordiameterwithveniercalipers.Xenograftvolumesareestimatedusingthefollowingformula[(length×width2)/2].Oncetumorsreach75to100mm3,micearerandomizedtoreceiveeither50mg/kgofML327orcontrolvehicle(70%polyethyleneglycol)viaintraperitonealinjectiontwicedailyfor14d.Weightandtumorvolumearerecordeddaily.Aftercompletionoftwoweeksoftreatment,miceareeuthanizedandtumorsareexcised,weighed,andRNAisisolated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellMolImmunol.2022Sep;19(9):1030-1041.•InflammBowelDis.2020Aug20;26(9):1340-1352.•ActaBiochBiophSin.2020Apr20;52(4):411-420.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•TechnolCancerResTreat.Jan-Dec2021;20:15330338211033077.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RellingerEJ,etal.IsoxazolecompoundML327blocksMYCexpressionandtumorformationinneuroblastoma.Oncotarget.2017Jul20;8(53):91040-91051.[2].AnH,etal.Smallmolecule/ML327mediatedtranscriptionalde-repressionofE-cadherinandinhibitionofepithelial-to-mesenchymaltransition.Oncotarget.2015Sep