BAY-11-7082-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEBAY11-7082Cat.No.:HY-13453CASNo.:19542-67-7分⼦式:C₁₀H₉NO₂S分⼦量:207.25作⽤靶点:IKK;Deubiquitinase;Autophagy;Apoptosis作⽤通路:NF-κB;CellCycle/DNADamage;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(482.51mM)扫描⼆维码，*"≥"meanssoluble,butsaturationunknown.运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM4.8251mL24.1255mL48.2509mL5mM0.9650mL4.8251mL9.6502mL10mM0.4825mL2.4125mL4.8251mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(12.06mM);Clearsolution此⽅案可获得≥2.5mg/mL(12.06mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。1/3www.MedChemEwww.MedChemE2.请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.5mg/mL(12.06mM);Clearsolution此⽅案可获得≥2.5mg/mL(12.06mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性BAY11-7082(BAY11-7821)⼀种IκBα磷酸化和NF-κB抑制剂，选择性且不可逆地抑制TNF-α诱导的IκB-α磷酸化，并减少NF-κB和粘附分⼦的表达。BAY11-7082抑制泛素特异性蛋⽩酶USP7和USP21(IC50分别为0.19,0.96μM)。BAY11-7082抑制脂质体中的gasderminD(GSDMD)孔形成以及炎性体介导的细胞凋亡和⼈和⼩⿏细胞中IL-1β的分泌。IC50&TargetNF-κBUSP7USP21Autophagy0.19μM(IC50)0.96μM(IC50)体外研究BAY11-7082(BAY11-7821),aninhibitorofNF-κB,inducesapoptosisofHTLV-I-infectedT-celllinesbutonlynegligibleapoptosisofHTLV-I-negativeTcells.Bay11-7082rapidlyandefficientlyreducestheDNAbindingofNF-κBinHTLV-I-infectedT-celllinesanddown-regulatedtheexpressionoftheantiapoptoticgene,Bcl-xL,regulatedbyNF-κB.Bay11-7082selectivelyinhibitsTax-inducedNF-κBactivityinahumanT-cellline[1].BAY11-7082inhibitsNFκBsignallingandisrecentlyshowntoinhibitthemajorityofE2andE3ligasestestedbyreactingcovalentlywiththecatalyticcysteineresidues.Moreover,BAY11-7082alsoinhibitsseveraltyrosinephosphatasesbyreactingwithcatalyticCysresidueoftheseenzymes.NSC697923isoriginallyshowntoinhibittheE2ligaseUbc13-Uev1A[2].BAY11-7082inhibitsthephosphorylationofIκBαandactivationofNF-κB,inducesthedeathofHBL-1cells.BAY11-7082completelysuppressestheLPS-stimulatedandIL-1-stimulatedphosphorylationoftheactivationloopofIKKβ[3].BAY11-7082actsbyinhibitingTNF-α-inducedphosphorylationofIκB-α,resultingindecreasedNF-κBanddecreasesexpressionofadhesionmolecules[4].体内研究BAY11-7082(2.5mg/kgand5mg/kg;intratumoralinjection;twice-weeklyfor21days)significantlysuppressestumorgrowthinadose-dependentmanner[6].AnimalModel:Four-week-oldmaleBALB/cnudemicewithhumangastriccarcinomacelllinesHGC-27[6]Dosage:Low-dose(2.5mg/kgbodyweight),high-dose(5mg/kgbodyweight)Administration:Intratumoralinjection;twice-weeklyfor21daysResult:Suppressedtumorgrowthinadose-dependentmanner.户使⽤本产品发表的科研⽂献•Gut.2018Nov;67(11):2035-2044.2/3www.MedChemEwww.MedChemE•CircRes.2020Mar13;126(6):e15-e29.•JImmunotherCancer.2020Nov;8(2):e001392.•JImmunotherCancer.2019Jul12;7(1):178.•CellMolImmunol.2020Jan3.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MoriN,etal.Bay11-7082inhibitstranscriptionfactorNF-kappaBandinducesapoptosisofHTLV-I-infectedT-celllinesandprimaryadultT-cellleukemiacells.Blood.2002Sep1;100(5):1828-1834.[2].RitortoMS,etal.ScreeningofDUBactivityandspecificitybyMALDI-TOFmassspectrometry.NatCommun.2014Aug27;5:4763.[3].StricksonS,etal.Theanti-inflammatorydrugBAY11-7082suppressestheMyD88-dependentsignallingnetworkbytargetingtheubiquitinsystem.BiochemJ.2013May1;451(3):427-437.[4].PierceJW,etal.Novelinhibitorsofcytokine-inducedIkappaBalphaphosphorylationandendothelialcelladhesionmoleculeexpressionshowanti-inflammatoryeffectsinvivo.JBiolChem.1997Aug22;272(34):21096-103.[5].JunJacobHu,etal.IdentificationofpyroptosisinhibitorsthattargetareactivecysteineingasderminD.ThePreprintServerForBiology,2018,Jul.10.[6].ChenL,etal.BAY11-7082,anuclearfactor-κBinhibitor,inducesapoptosisandSphasearrestingastriccancercells.JGastroenterol.2014May;49(5):864-74.McePdfHeight关注MCE中国公众号，

获取前沿资讯、最新活动和