GSK2807-Trifluoroacetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2807TrifluoroacetateCat.No.:HY-104009ACASNo.:2245255-66-5分⼦式:C₂₁H₃₃F₃N₈O₇分⼦量:566.53作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics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:≥250mg/mL(441.28mM)H2O:≥50mg/mL(88.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7651mL8.8257mL17.6513mL5mM0.3530mL1.7651mL3.5303mL10mM0.1765mL0.8826mL1.7651mL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:≥2.08mg/mL(3.67mM);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:≥2.08mg/mL(3.67mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.67mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:100mg/mL(176.51mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性GSK2807TrifluoroacetateSMYD3有效的、有选择性的，SAM竞争性抑制剂，其Ki值为14nM，IC50为130nM。IC50&TargetSMYD3SMYD314nM(Ki)130nM(IC50)体外研究Ahigh-resolutioncrystalstructurerevealsthatGSK2807bridgesthegapbetweentheSAM-bindingpocketandthesubstratelysinetunnelofSMYD3.GSK2807is24-foldselectiveforSMYD3incomparisonwiththecloselyrelatedenzymeSMYD2(Ki=14±6nMand345±36nM,respectively)[1].REFERENCES[1].VanAllerGS,etal.Structure-BasedDesignofaNovelSMYD3InhibitorthatBridgestheSAM-andMEKK2-BindingPockets.Structure.2016May3;24(5):774-781.[2].KaniskanHÜ,etal.InhibitorsofProteinMethyltransferasesandDemethylases.ChemRev.2018Feb14;118(3):989-1068.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl