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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/10mM*1mL in DMSO
商品详细Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/10mM*1mL in DMSO
Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/10mM*1mL in DMSO
Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/10mM*1mL in DMSO
商品编号： HY-10256-10mM*1mLinDMSO
品牌： MedChemExp
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产地： 美国(厂家直采)
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产品分类： 小分子
公司分类： Small_molecule
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商品介绍
SB203580isap38MAPKinhibitorwithIC50of0.3-0.5μM,alsoblocksPKBphosphorylationwithIC50of3-5μM.

CustomerValidation

  • •CellDeathDiffer.2017Mar;24(3):492-499.
  • •Elife.2016Apr11;5.pii:e14087.
  • •Oncogene.2017Apr;36(15):2095-2104.
  • •FrontImmunol.2017Oct10;8:1278.
  • •CancerLett.2017Feb16;393:22-32.
  • •CellDeathDis.2016Jun23;7(6):e2273.
  • •JMolCellCardiol.2015Dec;89(PtB):268-79.
  • •FreeRADIcBiolMed.2017Jul9;112:49-59.
  • •HumMolGenet.2017Sep15;26(18):3553-3563.
  • •ActaPhysiol(Oxf).2017Jul18.
  • •OxidMedCellLongev.2017;2017:6175841.
  • •SciRep.2017Oct19;7(1):13571.
  • •CellSignal.2016Feb;28(2):81-93.
  • •Virology.2017May22;508:150-158.
  • •MolImmunol.2017May4;87:161-170.
  • •ActaPharmacolSin.2017Aug;38(8):1120-1128.
  • •BiochemCellBiol.2017Feb;95(1):64-68.
  • •IntJClinExpMed.2017;10(9):13542-13549.
  • •BiomedicalResearch2017;28(8):3383-3386
  • •ManchesterMetropolitanUniversity.09May2017.
  • •ChinArchOtolaryngolHeadNeckSurg.2016Jan,23(1).
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

SB203580isap38MAPKinhibitorwithIC50of0.3-0.5μM,alsoblocksPKBphosphorylationwithIC50of3-5μM.

IC50&Target

IC50:0.3-0.5μM(p38MAPK)[1]

InVitro

SB203580inhibitsIL-2-drivenTcellproliferationwithanIC50of3-5μM,SB203580isabletoinhibittheactivityofPDK1inadose-dependentmannerwithanIC50inthe3-10μMrange[1].SB203580ataconcentrationof1μMissufficientforinhibitingp38kinaseactivityinTF-1cells.SB203580at5and10μMenhancesNF-κB-mediatedgenetranscriptionindependentlyofphosphorylationonthetransactivationdomainsofthep65subunit.SB203580at10μMenhancesphosphorylationofERK1/2andJNK[1].

InVivo

SB203580decreasesproteinconcentrationsofIL-1βfrom106.49±10.93to67.85±7.39pg/mLandTNF-αfrom462.54±50.16to252.71±44.03pg/mL.Similarly,theproteinlevelsofMMP-2andMMP-9aresignificantlylowerintheSB203580thantheEMgroup.AftertreatmentwithSB203580,theproteinlevelsofMMP-2andMMP-9decreasesfrom2.70±0.14to1.74±0.26ng/mLandfrom3.17±0.31to1.98±0.24ng/mL,respectively[3].SB203580isevaluatedinseveralmodelsofcytokineinhibitionandinflammatorydisease.ItisdemonstratedclearlytobeapotentinhibitorofinflammatorycytokineproductioninbothmiceandratswithIC50valuesof15to25mg/kg[4].

References

  • [1].LaliFV,etal.ThepyridinylimidazoleinhibitorSB203580blocksphosphoinositide-dependentproteinkinaseactivity,proteinkinaseBphosphorylation,andretinoblastomahyperphosphorylationininterleukin-2-stimulatedTcellsindependentlyofp38mitoge

    [2].BirkenkampKU,etal.Thep38MAPkinaseinhibitorSB203580enhancesnuclearfactor-kappaBtranscriptionalactivitybyanon-specificeffectupontheERKpathway.BrJPharmacol.2000Sep;131(1):99-107.

    [3].ZhouWD,etal.SB203580,ap38mitogen-activatedproteinkinaseinhibitor,suppressesthedevelopmentofendometriosisbydown-regulatingproinflammatorycytokinesandproteolyticfactorsinamousemodel.HumReprod.2010Dec;25(12):3110-6.

    [4].BadgerAM,etal.PharmacologicalprofileofSB203580,aselectiveinhibitorofcytokinesuppressivebindingprotein/p38kinase,inanimalmodelsofarthritis,boneresorption,endotoxinshockandimmunefunction.JPharmacolExpTher.1996Dec;279(3):1453-61.

    [5].LinY,etal.Criticalroleofastrocyticinterleukin-17 Ainpost-strokesurvivalandneuronaldifferentiationofneuralprecursorcellsinadultmice.CellDeathDis.2016Jun23;7(6):e2273.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.6495mL13.2475mL26.4950mL
5mM0.5299mL2.6495mL5.2990mL
10mM0.2649mL1.3247mL2.6495mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

SB203580isdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[2].

Phosphorylationofp38,JNK1/2,andERK1/2isanalysedbyWesternblotting.Briefly,TF-1cellsareculturedfor16hinRPMI1640containing0.1%FBSandsubsequentlystimulatedforvariousperiodsoftimewithmediumorOA(30ng/mL)orSB203580(1μM,5μM,10μM)plusOA.Afterharvesting,totalcellextractsarepreparedbyresUSPendingthecellsin500μL1×samplebuffer(containing2%SDS,10%glycerol,2%β-mercaptoethanol,60mMTris-HCl(pH6.8)andbromophenolblue)andlysingthecellsbypassingthemthrougha23G1needle(threetimes).Cellextractsaredirectlyboiledfor10minandstoredat-20°C.Beforeloading,samplesareagainboiledfor5minandcellextractsareresolvedbyrunning1/10thvolumeonaSDS/12.5%PAGEgel(acryla-mide:bisacrylamideis173:1)andtransferredtocellulosenitratemembrane.Immunoblottingwiththeantibodiesisperformedbystandardproceduresanddetectionisperformed[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[3]

SB203580isdissolvedinvehicle(PBS)(Mice)[3].

Mice[3]
ThirtyfemaleBALB/cmicewithexperimentallyinducedEMarerandomlydividedintotwogroups.Thefirstgroupisdesignatedasthestudygroup(SB203580group,n=15),whichisinjectedi.p.withSB203580atadoseof1μg/mgonadailybasis(thisdoseisestablishedinapre-test).Thesecondgroupisthepositivecontrolgroup(EMgroup,n=15),whichreceivednomedicationexcepti.p.injectionofisotonicsalinesolution(volumeequaltothatofSB203580).Thesham-operatedmiceservedasthenegativecontrols(sham-operatedgroup,n=15),whichreceivednomedicationbutdidhaveani.p.injectionofisotonicsalinesolution(volumeequaltothatofSB203580).TheinjectionofvehicleorSB203580started3daysbeforeinjectionoftheendometrialfragments(inSB203580andEMgroups)orthePBS(insham-operatedgroup)andlastedfor24days.Then,themicearesacrificedbycervicaldislocationonthedayofthelastinjectionandsurgicalproceduresareperformedunderasepticconditions.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LaliFV,etal.ThepyridinylimidazoleinhibitorSB203580blocksphosphoinositide-dependentproteinkinaseactivity,proteinkinaseBphosphorylation,andretinoblastomahyperphosphorylationininterleukin-2-stimulatedTcellsindependentlyofp38mitoge

    [2].BirkenkampKU,etal.Thep38MAPkinaseinhibitorSB203580enhancesnuclearfactor-kappaBtranscriptionalactivitybyanon-specificeffectupontheERKpathway.BrJPharmacol.2000Sep;131(1):99-107.

    [3].ZhouWD,etal.SB203580,ap38mitogen-activatedproteinkinaseinhibitor,suppressesthedevelopmentofendometriosisbydown-regulatingproinflammatorycytokinesandproteolyticfactorsinamousemodel.HumReprod.2010Dec;25(12):3110-6.

    [4].BadgerAM,etal.PharmacologicalprofileofSB203580,aselectiveinhibitorofcytokinesuppressivebindingprotein/p38kinase,inanimalmodelsofarthritis,boneresorption,endotoxinshockandimmunefunction.JPharmacolExpTher.1996Dec;279(3):1453-61.

    [5].LinY,etal.Criticalroleofastrocyticinterleukin-17 Ainpost-strokesurvivalandneuronaldifferentiationofneuralprecursorcellsinadultmice.CellDeathDis.2016Jun23;7(6):e2273.

MolecularWeight

377.43

Formula

C₂₁H₁₆FN₃OS

CASNo.

152121-47-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥33mg/mL

SB203580isdissolvedin1%DMSOat1 mg/mL[5].

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

References

  • [1].LaliFV,etal.ThepyridinylimidazoleinhibitorSB203580blocksphosphoinositide-dependentproteinkinaseactivity,proteinkinaseBphosphorylation,andretinoblastomahyperphosphorylationininterleukin-2-stimulatedTcellsindependentlyofp38mitoge

    [2].BirkenkampKU,etal.Thep38MAPkinaseinhibitorSB203580enhancesnuclearfactor-kappaBtranscriptionalactivitybyanon-specificeffectupontheERKpathway.BrJPharmacol.2000Sep;131(1):99-107.

    [3].ZhouWD,etal.SB203580,ap38mitogen-activatedproteinkinaseinhibitor,suppressesthedevelopmentofendometriosisbydown-regulatingproinflammatorycytokinesandproteolyticfactorsinamousemodel.HumReprod.2010Dec;25(12):3110-6.

    [4].BadgerAM,etal.PharmacologicalprofileofSB203580,aselectiveinhibitorofcytokinesuppressivebindingprotein/p38kinase,inanimalmodelsofarthritis,boneresorption,endotoxinshockandimmunefunction.JPharmacolExpTher.1996Dec;279(3):1453-61.

    [5].LinY,etal.Criticalroleofastrocyticinterleukin-17 Ainpost-strokesurvivalandneuronaldifferentiationofneuralprecursorcellsinadultmice.CellDeathDis.2016Jun23;7(6):e2273.

Purity:99.54%