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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 | ||||||||||||
Storage |
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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%
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westblot蛋白免疫印迹实验跑小分子蛋白(15kd)条带一直是波浪状,有人说是胶的问题,可同时跑了36kd蛋白,条带是直的,有人说是要恒流跑,电压不要太大,我的转膜条件是50v,50min,请教各位大神指点,万分感谢!!!
如题,之前没做过药代,老师给了一个600+Da的五肽,想测下药代动参数,看文献推荐上述两种方法,但是不知道选哪种更好,lcms前处理会不会影响小肽。
求助各位前辈,我最近在合成的化合物水溶性很好,非常好,以至于可以随便溶解在水里,它的六氟磷酸盐也可以随意溶解在水里(大于50uM),细胞成像实验显示它根本进不去细胞,求问有没有啥方法包裹一下让它进去?我搜了一下文献,感觉多数是把脂溶性特别好的东西包裹一下弄进去的,也许是搜索姿势不对没找到我需要的答案,**点拨啊!!!
求助各位大神,现在想购买小分子数据库,求大神推荐。
我知道的免费的数据库有zinc
求推荐哪家公司或者研究所的小分子数据库可以购买,十分感谢!!!!!!
有机的是有机化合物的简称,它指的是含碳化合物.
但是,有四大类常见物质一般不作为有机物处理:
1、碳的氧化物,如CO和CO2.
2、碳酸及其盐,如CaCO3.
3、金属碳化物,如CaC2.
4、拟卤素及其化合物,如(CN)2与KSCN.
水的化学式为H2O,它不含有碳元素,故不是有机物.
但若所描述的水不是化学意义的水,而是自然界存在的天然水,那么,水中会溶有一定量的有机物.
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