HOIPIN-8-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHOIPIN-8Cat.No.:HY-122882分?式:C??H??F?N?NaO?分?量:456.38作?靶點(diǎn):E1/E2/E3Enzyme作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(54.78mM;ultrasonicandadjustpHto2withHCl)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1912mL10.9558mL21.9116mL5mM0.4382mL2.1912mL4.3823mL10mM0.2191mL1.0956mL2.1912mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性HOIPIN-8線性泛素鏈組裝復(fù)合物(LUBAC)的有效抑制劑，IC50為11nM。HOIPIN-8HOIPIN-1的衍?物，與HOIPIN-1相?，它表現(xiàn)出255倍的petit-LUBAC抑制能?，對(duì)LUBAC和TNF-α介導(dǎo)的NF-κB激活作?的抑制，HOIPIN-1抑制作?的10倍和4倍。HOIPIN-8?個(gè)很有前途的?具?于研究LUBAC的細(xì)胞功能。體外研究HOIPIN-8(0-100μM;72hours)haslittlecelltoxicityonA549cells,andexhibitsanIC50valueof100μM[1].HOIPIN-8(0-10μM;24hours)hasaninhibitoryeffectover10-foldenhancementoverthatofHOIPIN-1onNF-κBactivation,exhibitsanIC50valueof0.42?μMinHEK293Tcells[1].HOIPIN-8(0-30μM;NF-κ1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBluciferasereporteristransfectedintocellsfor18hours;thenwith10?ng/mlTNF-αfor6?h)exhibitsa4-foldenhancementsofthepotencythanHOIPIN-1,theIC50valueis11.9μM.ItalsoeffectivelyreducesIL-1β-inducedexpressionofNF-κBtargetgenes,suchasICAM1andIL-6ascomparedtoHOIPIN-1[1].CellViabilityAssay[1]CellLine:HumanlungcarcinomaA549?cells,HEK293TcellsConcentration:0μM;1μM;3μM;10μM;30μM;100μMIncubationTime:72hoursResult:DidnoteffectA549?cellviability.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