JQEZ5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJQEZ5Cat.No.:HY-100846CASNo.:1913252-04-6分⼦式:C₃₀H₃₈N₈O₂分⼦量:542.68作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(46.07mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8427mL9.2135mL18.4271mL5mM0.3685mL1.8427mL3.6854mL10mM0.1843mL0.9214mL1.8427mL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%salineSolubility:≥2.5mg/mL(4.61mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性JQEZ5⼀种有效的选择性的EZH2赖氨酸甲转移酶抑制剂。JQEZ5以SAM竞争性⽅式抑制PRC2的酶功能，IC50为80nM。JQEZ5具有抗肿瘤作⽤。IC50&TargetEZH2[1]体外研究JQEZ5inhibitsenzymaticfunctionalityofPRC2withabiochemicalIC50of80nM.JQEZ5exhibitsS-adenosylmethionine(SAM)-competitiveinhibitionofPRC2[1].H661cellstreatedwithincreasingconcentrationsofJQEZ5demonstrateacutelyreducedlevelsofH3K27me3withoutaffectingH3K27mono-ordi-methylation.JQEZ5suppressestheproliferationofEZH2-overexpressingH661andH522cellsaftertreatmentfor4dayswithoutaffectingtheproliferationofcelllinesthatweredeemedinsensitivetoEZH2knockdown[1].体内研究JQEZ5(75mg/kg;intraperitonealinjection;daily;for3weeks)treatmentexhibitsrapidandpronouncedtumorregressionoverthethreeweektreatmentcourse.AndH3K27me3levelsarelargelyreducedwithtreatmentfurtherconfirmingtheon-targeteffectofJQEZ5inmice[1].PROTOCOLAnimalTumor-bearinggenetically-engineeredmousemodels(GEMMs)aremonitoredforonsetofsymptoms(breathAdministration[1]distress)andthentreatedwithJQEZ5forthreeweeks(75mg/kgIPdaily).TumorsarevisualizedbyMRIandtumorvolumeofthelungsiscalculatedusing3DSlicer.Forxenograftexperiments,H661cellsaredissociatedintosinglecells,countedandresuspendedat2×106cellsper250µLof1:1media/matrigel.Eight-to12-week-oldfemaleFoxn1nu/Foxn1numiceareinjectedsubcutaneouslywith2×106cellsintwotothreespotsontheflanks.Tumorsareallowedtogrowtoanapproximatesizeof200mm3(~10weeks)andthemicearerandomizedforvehicle(n=3)orJQEZ5administration(n=6,75mg/kg/d,i.p.)for18days.Tumorgrowthismeasuredbycalipermeasurementsandtumorvolumeiscalculatedbystandardmethods[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JTranslMed.2019Nov11;17(1):366.•ActaPharmacolSin.2021Apr13.•Gene.2022Feb16;822:146317.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangH,etal.OncogenicDeregulationofEZH2asanOpportunityforTargetedTherapyinLungCancer.CancerDiscov.2016Sep;6(9):1006-21.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfully