ML240-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML240Cat.No.:HY-19795CASNo.:1346527-98-7分⼦式:C₂₃H₂₀N₆O分⼦量:396.44作⽤靶点:p97作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:12.5mg/mL(31.53mM;Needultrasonic)Ethanol:<1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5224mL12.6122mL25.2245mL5mM0.5045mL2.5224mL5.0449mL10mM0.2522mL1.2612mL2.5224mL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:2.5mg/mL(6.31mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.31mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.31mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ML240⼀种有效的p97抑制剂，抑制p97ATPase，IC50值为100nM。IC50&TargetIC50:100nM(p97)[1]体外研究ML240isapotentp97inhibitor,withanIC50of100nM.ML240isactiveintheUbG76V-GFPstabilizationassay(IC50,0.9μM).ML240inhibitsp97competitivelywithrespecttoATPwithaKivaluesof0.22μM.ML240alsoinhibitslabelingofonlythreeproteinkinasedomainsby>50%whentestedat20μM:PIP5K3(belongstophosphoinositide-3kinasefamily),JAK1JH2(N-terminalpseudokinasedomainofJAK1),andDNAPK(DNA-dependentproteinkinase).ML240(1.1,3.3,10,or20μM)inducesexecutionercaspases3and7andtriggerscelldeathindependentlyofapicalcaspases8and9[1].ML240iscytotoxictoHCT15andSW403cells,withGI50sof0.76and0.5μMaftertreatmentfor24h,and0.54and0.5μMaftertreatmentfor72h,respectively[2].PROTOCOLCellAssay[2]HeLacellsstablyexpressingODD-luciferaseareseededontoa96-wellwhitesolidbottomplate(5000cells/well)andcellsaregrownfor16h.CellsaretreatedwithDMEMcontainingMG132(4μM)for1handwashedwith100μLPBStwice.DMEMcontaining2.5%FBS,cycloheximide(50μg/mL)andML240areaddedintothewell.Four96-wellplatesarepreparedandoneoftheplatesistakenoutfromincubatorateachtimepoint(70,90,120,or150min).Luciferin(50μLof1mg/mLinPBS)isaddedintoeachwellcontaining50μLofmediumandincubatedatroomtemperaturewithshakingat500rpmfor5min.Luminescenceintensityisdeterminedwith0.1msintegrationtimeontheSynergyHTMicroplateReader[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•PLoSOne.2021Nov3;16(11):e0251957.•VetMicrobiol.2022Jul12;272:109511.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].ChouTFetal.Structure-activityrelationshipstudyrevealsML240andML241aspotentandselectiveinhibitorsofp97ATPase.ChemMedChem,2013Feb,8(2):297-312.[2].ChouTF,etal.Selective,reversibleinhibitorsoftheAAAATPasep97.ProbeReportsfromtheNIHMolecularLibrariesProgram.April14,2011.McePdfHeightCaution:Producthasnotb