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HY-12041-10mM*1mLinDMSO
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SP600125isabroad-spectrumJNKinhibitorforJNK1,JNK2andJNK3withIC50of40nM,40nMand90nM,respectively.

CustomerValidation

  • •Biomaterials.2017Mar22;130:14-27.
  • •CellDeathDiffer.2017Mar;24(3):492-499.
  • •Elife.2016Apr11;5.pii:e14087.
  • •JAutoimmun.2017Nov20.pii:S0896-8411(17)30612-1.
  • •FrontImmunol.2017Oct10;8:1278.
  • •CancerLett.2017Feb16;393:22-32.
  • •CellMolLifeSci.2017Oct25.
  • •JMolCellCardiol.2015Dec;89(PtB):268-79.
  • •FreeRADIcBiolMed.2017Jul9;112:49-59.
  • •Oncotarget.2016Dec20;7(51):85079-85096.
  • •OxidMedCellLongev.2017;2017:7426458.
  • •OxidMedCellLongev.2017;2017:6175841.
  • •CellSignal.2016Feb;28(2):81-93.
  • •MolImmunol.2017May4;87:161-170.
  • •ChemBiolInteract.2017Nov1;277:62-73.
  • •IntJMolMed.2017Jul;40(1):164-174.
  • •IntJMolMed.2017Jan;39(1):71-80.
  • •UniversitätWürzburg.2016-4-27.
  • •HarvardMedicalSchoolLINCSLIBRARY
  • •ThirdMilitaryMedicalUniversity
Description

SP600125isabroad-spectrumJNKinhibitorforJNK1,JNK2andJNK3withIC50of40nM,40nMand90nM,respectively.

IC50&Target

IC50:40/40/90nM(JNK1/2/3)[1]

InVitro

SP600125isanATP-competitiveinhibitorofJNK2withaKivalueof0.19±0.06μM.SP600125inhibitsthephosphorylationofc-JunwithIC50of5μMto10μMinJurkatTcells.InCD4+cells,suchasTh0cellsisolatedfromeitherhumancordorperipheralblood,SP600125blockscellactivationanddifferentiationandinhibitstheexpressionofinflammatorygenesCOX-2,IL-2,IL-10,IFN-γ,andTNF-α,withIC50of5μMto12μM[1].InamousebetacellsMIN6,SP600125(20μM)inducesthephosphorylationofp38MAPKanditsdownstreamCREB-dependentpromoteractivation[2].InHCT116cells,SP600125(20μM)blockstheG2phasetomitosistransitionandinducesendoreplication.ThisABIlityofSP600125isindependentofJNKinhibition,butduetoitsinhibitionofCDK1-cyclinBactivationupstreamofAuroraAandPolo-likekinase1[3].

InVivo

AdmiNISTrationofSP600125at15or30mg/kgi.v.significantlyinhibitsTNF-αserumlevels,whereasoraladministrationdose-dependentlyblocksTNF-αexpressionwithsignificantinhibitionobservedat30mg/kgperos[1].SP600125attenuatesLPS-inducedALIinratsinvivo.TheexpressionlevelsofTNF-αandIL-6intheBALFinratsintheSP600125grouparesignificantlydecreased[4].

References

  • [1].BennettBL,etal.SP600125,ananthrapyrazoloneinhibitorofJunN-terminalkinase.ProcNatlAcadSciUSA,2001,98(24),13681-13686.

    [2].VaishnavD,etal.SP600125,aninhibitorofc-junN-terminalkinase,activatesCREBbyap38MAPK-mediatedpathway.BiochemBiophysResCommun,2003,307(4),855-860.

    [3].KimJA,etal.SP600125suppressesCdk1andinducesendoreplicationdirectlyfromG2phase,independentofJNKinhibition.Oncogene,2010,29(11),1702-1716.

    [4].ZhengY,etal.JNKinhibitorSP600125protectsagainstlipopolysaccharide-inducedacutelunginjuryviaupregulationofclaudin-4.ExpTherMed.2014Jul;8(1):153-158.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM4.5407mL22.7035mL45.4071mL
5mM0.9081mL4.5407mL9.0814mL
10mM0.4541mL2.2704mL4.5407mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

SP600125isdissolvedinDMSO(20mM)andstored,andthendilutedwithappropriatemedia(DMSO0.1%)beforuse[1].

DeterminationofmRNAhalf-lifeisperformedessentially,exceptthatCD14+cellsarestimulatedwith(bacterial)lipopolysaccharide(LPS;50ng/mL)for2hbeforeadditionofactinomycinD(5μg/mL).SP600125(25μM)orvehicle(0.5%DMSOvol/vol)isaddedimmediatelyfollowingtheactinomycinD.Analysisisperformedbyusingreal-timereversetranscription(RT)-PCR.TotalRNAisextractedwithanRNeasyMinikit.TNFmRNAismeasuredbyrealtimeRT-PCR,usingaTNFTaqmanprobe.Alldataarenormalizedbyusingglyceraldehyde-3-phosphatedehydrogenase(GAPDH)expression.TheTNF-αforwardprimeris5′-CTGGCCCAGGCAGTCAGAT-3′andthereverseprimeris5′-TATCTCTCAGCTCCACGCCATT-3′.TheTaqmanprobesequenceis5′-FAM-CCTGTAGCCCATGTTGTAGCAAACCCTCA-TAMRA-3′[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1][4]

SP600125isdissolvedin30%PEG-400/20%polypropyleneglycol/15%CremophorEL/5%ethanol/30%saline(Mice)[1].

Mice[1]
FemaleCD-1mice(8-10weeksofage)aredosedi.v.orperoswithSP600125inPPCESvehicle(30%PEG-400/20%polypropyleneglycol/15%CremophorEL/5%ethanol/30%saline),finalvolumeof5mL/kg,15minbeforei.v.injectionwithLPSinsaline(0.5mg/kg).At90min,aterminalbleedisobtainedfromtheaBDominalvenacava,andtheserumisrecovered.SamplesareanalyzedformouseTNF-αbyusinganELISA.
Rat[4]
Atotalof40maleWistarratsarerandomlydividedintofourgroups(n=10):thecontrolgroup,LPSgroup,normalsalinegroup(NS)andtheSP600125group.Acutelunginjury(ALI)isinducedviaintratrachealinjectionofLPS.Briefly,theratsareanesthetizedwithpentobarbitalsodiumfollowedbyintratrachealinjectionof5mg/kgLPS.Theratsarethenplacedinaverticalpositionandrotatedfor1mintodistributetheLPSinthelungs.NormalsalineorSP600125isadministeredviaintraperitonealinjection(15mg/kg)10minaftertheLPSinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].BennettBL,etal.SP600125,ananthrapyrazoloneinhibitorofJunN-terminalkinase.ProcNatlAcadSciUSA,2001,98(24),13681-13686.

    [2].VaishnavD,etal.SP600125,aninhibitorofc-junN-terminalkinase,activatesCREBbyap38MAPK-mediatedpathway.BiochemBiophysResCommun,2003,307(4),855-860.

    [3].KimJA,etal.SP600125suppressesCdk1andinducesendoreplicationdirectlyfromG2phase,independentofJNKinhibition.Oncogene,2010,29(11),1702-1716.

    [4].ZhengY,etal.JNKinhibitorSP600125protectsagainstlipopolysaccharide-inducedacutelunginjuryviaupregulationofclaudin-4.ExpTherMed.2014Jul;8(1):153-158.

MolecularWeight

220.23

Formula

C₁₄H₈N₂O

CASNo.

129-56-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥45mg/mL

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

Purity:98.69%

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