LLY-507-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELLY-507Cat.No.:HY-19313CASNo.:1793053-37-8分⼦式:C₃₆H₄₂N₆O分⼦量:574.76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:15mg/mL(26.10mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7399mL8.6993mL17.3986mL5mM0.3480mL1.7399mL3.4797mL10mM0.1740mL0.8699mL1.7399mL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(4.35mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LLY-507⼀种有效、选择性的赖氨酸甲转移酶SMYD2抑制剂。LLY-507能有效抑制SMYD2甲化p53肽的能⼒，其IC50[1]。IC50&TargetSMYD250)体外研究LLY-507is>100-foldselectiveforSMYD2over21othermethyltransferasesincludingSMYD3[1].LLY-507bindstothesubstratechannelofSMYD2andsupportstheselectivityofitsinhibition[1].LY-507isabletopotentlyinhibitthemethylationofH4peptidebySMYD2enzymewithanIC50of31nM[1].LLY-507(0.03-20μM;28hours)inhibitsSMYD2-mediatedmethylationofp53Lys370inU2OScells,withanIC50of0.6μM[1].LLY-507(0-20μM;3-7days)inhibitstheproliferationofseveralESCC,HCC,andbreastcancercelllines[1].CellProliferationAssay[1]CellLine:ESCC,HCC,breastcancercelllinesConcentration:0-20μMIncubationTime:3days,7daysResult:Inhibitedtumorcellproliferation.WesternBlotAnalysis[1]CellLine:HEK293cellsConcentration:0.03μM,0.07μM,0.15μM,0.3μM,0.6μM,1.25μM,2.5μMIncubationTime:28hoursResult:InhibitedSMYD2-mediatedmethylationofp53Lys370incells.户使⽤本产品发表的科研⽂献•CellDeathDis.2022Oct21;13(10):890.•CellDeathDis.2018Jan26;9(2):129.•Cells.2022Apr8;11(8):1262.•CellDeathDiscov.2022Jun6;8(1):274.•Development.2020Sep28;147(18):dev190678.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].NguyenH,etal.LLY-507,aCell-active,Potent,andSelectiveInhibitorofProtein-lysineMethyltransferaseSMYD2.JBiolChem.2015May29;290(22):13641-13653.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati