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Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/200mg

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Medchemexpress/SB 203580(Synonyms: RWJ 64809)/HY-10256/200mg

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MedChemExpress

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HY-10256-10mM*1mLinDMSO

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4000-520-616

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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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.6495mL	13.2475mL	26.4950mL
5mM	0.5299mL	2.6495mL	5.2990mL
10mM	0.2649mL	1.3247mL	2.6495mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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%

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