MZP-54-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMZP-54Cat.No.:HY-112376CASNo.:2010159-47-2分⼦式:C₅₅H₆₆ClN₇O₉S分⼦量:1036.67作⽤靶点:PROTACs;EpigeneticReaderDomain作⽤通路:PROTAC;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Ethanol:50mg/mL(48.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9646mL4.8231mL9.6463mL5mM0.1929mL0.9646mL1.9293mL10mM0.0965mL0.4823mL0.9646mL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%EtOH>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.41mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.41mM);Clearsolution3.请依序添加每种溶剂：10%EtOH>>90%cornoilSolubility:≥2.5mg/mL(2.41mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MZP-54由vonHippel-Lindau配体和BRD3/4配体相连的PROTAC，对Brd4BD2的Kd值为4nM。IC50&TargetVHLBRD4BD24nM(Kd)体外研究MZP-54isaselectivedegraderofBRD3/4basedonPROTACtechnology,withaKdof4nMforBrd4BD2.MZP-54bindstoVHL-EloC-EloBprotein(VCB)withaKdof105±24nM.MZP-54showsaninhibitoryactivityagainstMV4;11andHL60cells,withpEC50sof7.08±0.05and6.37±0.03,respectively.MZP-54alsoexhibitshighdepletionofcMyclevels[1].PROTOCOLCellAssay[1]MV4;11orHL60cellsareincubatedwithMZP-54atthedesiredconcentrationfor48honaclear-bottom384-wellplate.CellsarekeptinRPMImediumsupplementedwith10%FBS,l-glutamine,penicillin,andstreptomycin.Initialcelldensityis3×105permL.CellsaretreatedwithvariousconcentrationsofMZP-54or0.05%DMSO.Aftertreatment,cellviabilityismeasuredwithcellviabilityassaykit.Signalisrecorded.DataareanalyzedwithGraphpadPrismsoftwaretoobtainEC50valuesofeachMZP-54[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].ChanKH,etal.ImpactofTargetWarheadandLinkageVectoronInducingProteinDegradation:ComparisonofBromodomainandExtra-Terminal(BET)DegradersDerivedfromTriazolodiazepine(JQ1)andTetrahydroquinoline(I-BET726)BETInhibitorScaffolds.JMeMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications