Description | SB203580isap38MAPKinhibitorwithIC50of0.3-0.5μM,alsoblocksPKBphosphorylationwithIC50of3-5μM. |
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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]. |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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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] | ||||||||||||||||
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MolecularWeight | 377.43 | ||||||||||||
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Formula | C₂₁H₁₆FN₃OS | ||||||||||||
CASNo. | 152121-47-6 | ||||||||||||
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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="">1> | ||||||||||||
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Purity:99.54%