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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/海湾11-7082（同义词：海湾11-7821）/HY-13453/100mg
商品详细Medchemexpress/海湾11-7082（同义词：海湾11-7821）/HY-13453/100mg
Medchemexpress/海湾11-7082（同义词：海湾11-7821）/HY-13453/100mg
Medchemexpress/海湾11-7082（同义词：海湾11-7821）/HY-13453/100mg
商品编号： HY-13453-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
BAY11-7082isaNF-κBinhibitor.BAY11-7082inhibitsubiquitin-specificprotease(USP)7and21withanIC50of0.19 μMand0.96 μM,respectively.

CustomerValidation

  • •Gut.2017Sep12.pii:gutjnl-2017-314098.
  • •FrontImmunol.2017Oct10;8:1278.
  • •CellMolLifeSci.2017Oct25.
  • •EnvironPollut.2017Oct;229:964-975.
  • •EurJMedChem.2017Aug3;139:337-348.
  • •ToxicolApplPharmacol.2017Mar22;323:44-52.
  • •IntImmunopharmacol.2017Jun14;50:30-37.
  • •IntImmunopharmacol.2016Oct;39:149-57.
Description

BAY11-7082isaNF-κBinhibitor.BAY11-7082inhibitsubiquitin-specificprotease(USP)7and21withanIC50of0.19 μMand0.96 μM,respectively.

IC50&Target

NF-κB[1]
IC50:0.19 μM(USP7),0.96 μM(USP21)[2]

InVitro

Bay11-7082,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].

References

  • [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.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM4.8251mL24.1255mL48.2509mL
5mM0.9650mL4.8251mL9.6502mL
10mM0.4825mL2.4125mL4.8251mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[3]

UBE1(0.17μM)in22.5μLof20mMHepes,pH7.5,containing10μMubiquitinisincubatedfor45minat21°Cwith1μLofDMSOor1μLofBAY11-7082inDMSO.A2.5μLsolutionof10mMmagnesiumacetateand0.2mMATPisadded,incubatedfor10minat30°C,andthereactionsareterminatedbytheadditionof2.5μLof10%(w/v)SDSandheatingfor6minat75°C.ThesamplesaresubjectedtoSDS/PAGEintheabsenceofanythiol.Thegelsarestainedfor1hwithCoomassieInstantBlueanddestainedbywashingwithwater.TheloADIngofubiquitintoE2conjugatingenzymesiscarriedoutinanidenticalmanner,exceptthatUBE1(0.17μM)ismixedwithUbc13(2.4μM)orUbcH7(2.9μM)priortoincubationwithBAY11-7082[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

BAY11-7082isdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[1].

TheeffectofBay11-7082oncellgrowthisassayedbytheWST-1methodasdescribedpreviously.TheWST-1cellcountingkitisobtainedfromWakoChemicals.Briefly,2×104(celllines)or2×105(PBMCs)cellsareincubatedina96-wellmicrocultureplateundertheaboveconditionsintheabsenceorpresenceofvariousconcentrationsofBay11-7082.After48hoursofculture,10μLWST-1solutionisaddedandthecellsarefurtherincubatedforanother2hours.Thenumberofsurvivingcellsismeasuredwithamicroplatereaderatareferencewavelengthof655nmandtestwavelengthof450nm.CellviABIlityisdeterminedaspercentageofthecontrol(ie,absenceofBay11-7082)[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [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.

MolecularWeight

207.25

Formula

C₁₀H₉NO₂S

CASNo.

19542-67-7

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.64%