ML241-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML241hydrochlorideCat.No.:HY-19797ACASNo.:2070015-13-1分⼦式:C₂₃H₂₅ClN₄O分⼦量:408.92作⽤靶点:p97作⽤通路:CellCycle/DNADamage储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥34mg/mL(83.15mM)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4455mL12.2273mL24.4547mL5mM0.4891mL2.4455mL4.8909mL10mM0.2445mL1.2227mL2.4455mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥2.5mg/mL(6.11mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.11mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.11mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ML241hydrochloride⼀种有效的p97抑制剂，IC50值为100nM。IC50&TargetIC50:100nM(p97)[1]体外研究ML241hydrochlorideisapotentp97inhibitor,inhibitingp97ATPasewithIC50valuesof100nM.ML241inhibitsp97competitivelywithrespecttoATPwithaKivaluesof0.35μM.ML241(20μM)showsnoobviousinhibitionoftheappr170kinasestested.ML241stabilizesUbG76V-GFPwithIC50of3.5μM[1].ML241iscytotoxictoHCT15andSW403cells,withGI50sof53and33μMaftertreatmentfor24h,and13and12μMaftertreatmentfor72h,respectively[2].PROTOCOLCellAssay[2]HeLacellsstablyexpressingODD-luciferaseareseededontoa96-wellwhitesolidbottomplate(5000cells/well)andcellsaregrownfor16h.CellsaretreatedwithDMEMcontainingMG132(4μM)for1handwashedwith100μLPBStwice.DMEMcontaining2.5%FBS,cycloheximide(50μg/mL)andML241areaddedintothewell.Four96-wellplatesarepreparedandoneoftheplatesistakenoutfromincubatorateachtimepoint(70,90,120,or150min).Luciferin(50μLof1mg/mLinPBS)isaddedintoeachwellcontaining50μLofmediumandincubatedatroomtemperaturewithshakingat500rpmfor5min.Luminescenceintensityisdeterminedwith0.1msintegrationtimeontheSynergyHTMicroplateReader[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].ChouTF,etal.Structure-activityrelationshipstudyrevealsML240andML241aspotentandselectiveinhibitorsofp97ATPase.ChemMedChem.2013Feb;8(2):297-312.[2].ChouTF,etal.Selective,reversibleinhibitorsoftheAAAATPasep97.ProbeReportsfromtheNIHMolecularLibrariesProgram.April14,2011.McePdfHeightCaution:Producthasnotbeenfullyvalidated