MZP-54-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMZP-54Cat.No.:HY-112376CASNo.:2010159-47-2分?式:C??H??ClN?O?S分?量:1036.67作?靶點(diǎn):PROTACs;EpigeneticReaderDomain作?通路:PROTAC;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)Ethanol:50mg/mL(48.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.9646mL4.8231mL9.6463mL5mM0.1929mL0.9646mL1.9293mL10mM0.0965mL0.4823mL0.9646mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%EtOH>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.41mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.41mM);Clearsolution3.請依序添加每種溶劑：10%EtOH>>90%cornoilSolubility:≥2.5mg/mL(2.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性MZP-54由vonHippel-Lindau配體和BRD3/4配體相連的PROTAC，對Brd4BD2的Kd值為4nM。IC50&TargetVHLBRD4BD24nM(Kd)體外研究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