HOIPIN-8-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHOIPIN-8Cat.No.:HY-122882分⼦式:C₂₃H₁₅F₂N₄NaO₃分⼦量:456.38作⽤靶点:E1/E2/E3Enzyme作⽤通路:MetabolicEnzyme/Protease储存⽅式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:25mg/mL(54.78mM;ultrasonicandadjustpHto2withHCl)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1912mL10.9558mL21.9116mL5mM0.4382mL2.1912mL4.3823mL10mM0.2191mL1.0956mL2.1912mL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,awayfrommoistureandlight)。-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。BIOLOGICALACTIVITY⽣物活性HOIPIN-8线性泛素链组装复合物(LUBAC)的有效抑制剂，IC50为11nM。HOIPIN-8HOIPIN-1的衍⽣物，与HOIPIN-1相⽐，它表现出255倍的petit-LUBAC抑制能⼒，对LUBAC和TNF-α介导的NF-κB激活作⽤的抑制，HOIPIN-1抑制作⽤的10倍和4倍。HOIPIN-8⼀个很有前途的⼯具⽤于研究LUBAC的细胞功能。体外研究HOIPIN-8(0-100μM;72hours)haslittlecelltoxicityonA549cells,andexhibitsanIC50valueof100μM[1].HOIPIN-8(0-10μM;24hours)hasaninhibitoryeffectover10-foldenhancementoverthatofHOIPIN-1onNF-κBactivation,exhibitsanIC50valueof0.42ꢀμMinHEK293Tcells[1].HOIPIN-8(0-30μM;NF-κ1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBluciferasereporteristransfectedintocellsfor18hours;thenwith10ꢀng/mlTNF-αfor6ꢀh)exhibitsa4-foldenhancementsofthepotencythanHOIPIN-1,theIC50valueis11.9μM.ItalsoeffectivelyreducesIL-1β-inducedexpressionofNF-κBtargetgenes,suchasICAM1andIL-6ascomparedtoHOIPIN-1[1].CellViabilityAssay[1]CellLine:HumanlungcarcinomaA549ꢀcells,HEK293TcellsConcentration:0μM;1μM;3μM;10μM;30μM;100μMIncubationTime:72hoursResult:DidnoteffectA549ꢀcellviability.RT-PCR[1]CellLine:HEK293TcellsConcentration:0μM;0.3μM;1μM;10μM;30μMIncubationTime:24hoursResult:Hadaninhibitoryeffectontheinflammatorycytokine-inducedNF-κBactivationpathway.REFERENCES[1].KenKatsuya,etal.Small-moleculeInhibitorsofLinearUbiquitinChainAssemblyComplex(LUBAC),HOIPINs,SuppressNF-κBSignaling.BiochemBiophysResCommun.2019Feb12;509(3):700-706.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu