Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML327Cat.No.:HY-103038CASNo.:1883510-31-3分?式:C??H??N?O?分?量:366.37作?靶點(diǎn):c-Myc;Autophagy作?通路:Apoptosis;Autophagy儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:32mg/mL(87.34mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7295mL13.6474mL27.2948mL5mM0.5459mL2.7295mL5.4590mL10mM0.2729mL1.3647mL2.7295mL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。-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?。BIOLOGICALACTIVITY?物活性ML327MYC的阻斷劑，也可以去阻遏E-鈣粘蛋?轉(zhuǎn)錄和逆轉(zhuǎn)上?-間質(zhì)轉(zhuǎn)化(EMT)。IC50&TargetMYC[1]體外研究TreatmentwithML327inducesanelongatedmorphologyinneuroblastomacells.BE(2)-Ccellstreatedwith1/3MasterofBioactiveMolecules—您?邊的抑制劑?師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].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellMolImmunol.2022Sep;19(9):1030-1041.?InflammBowelDis.2020Aug20;26(9):1340-1352.?ActaBiochBiophSin.2020Apr20;52(4):411-420.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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