Formulation | H2O |
MolecularWeight | |
Storage | -80°C |
Purity | HPLCandTLCanalysis |
Compound | |
Assay | N/A |
ShelfLife(properlystored) | 12months |
ChemicalFormula | |
ThestructureofdansylarginineN-(3-ethyl-1,5-pentanediyl)amide(DAPA)isillustrated.DAPAisapotentinhibitorofthrombinwhichexhibitsuniquechangesinitsfluorescentpropertieswhenboundtothrombin.
Overview:
DansylarginineN-(3-ethyl-1,5-pentanediyl)amide,morecommonlyreferredtoasDAPA,isapotent(Ki=10-7M)andspecificsyntheticthrombininhibitor(1).OfspecialinterestaretheuniquefluorescentpropertiescontributedbythedansylmoietyofDAPA.Whenboundtothrombin,thefluorescenceintensityandlifetimeofthedansylmoietyareincreasedthreefold.Theenhancementoffluorescenceintensity,coupledwithitsinhibitoryproperties,havemadethiscompoundextremelyusefulforstudiesinvolvingthrombingeneration(2-7).Inadditiontoanincreaseinfluorescenceintensityandlifetime,thereisadecreaseindepolarizationoftheexcitationsignalwhichalsosupportsfluorescencepolarizationstudies.
TheinhibitorpropertiesofDAPAalonehavebeenusefulinavarietyofapplications.DAPAisroutinelyusedasaproteaseinhibitorduringtheisolationofproteinsthataresusceptIBLetothrombincleavage.FurThermore,byeliminatingthefeedbackofthrombinactivityduringprothrombinactivation,theisolationofreactionintermediatessuchasfragment1.2,andmeizothrombinhavebeenmadepossible(7).
DAPAissynthesizedaccordingtheproceduredescribedbyNesheim,etal.(1).HPLC,TLCandspectralanalysesareusedtodeterminethepurityofthefinalproduct.DAPAissuppliedinwater.Whenproperlystoredat-20°Candprotectedfromlight,thecompoundisstableformanyyears.
Properties:
Formula | C25H39O3N6S1Cl1(reference#1) DansylarginineN-(3-ethyl-1,5-pentanediyl)amide | |||||
---|---|---|---|---|---|---|
Molecularweight | 539g/mole(1) | |||||
Extinctioncoefficient |
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Specialproperties | Aspecificandpotentthrombininhibitor(Ki=10-7M).Exhibitsa3-foldincreaseinfluorescenceintensityandlifetimewhenboundtothrombin. |
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NaturalProteinStopsDeadlyHumanBrainCancerInMice
ScientistsfromJohnsHopkinsandfromtheUniversityofMilanhaveeffectivelyproventhattheycaninhibitlethalhumanbraincancersinmiceusingaproteinthatselectivelyinducespositivechangesintheactivityofcellsthatbehavelikecancerstemcells.ThereportispublishedinNature.
Themostcommontypeofbraincancer-glioblastoma-ismarkedbythepresenceofthesestem-cell-likebraincells,which,insteadoftriggeringthereplacementofdamagedcells,formcancertissue.Stemcells,unlikeallothercellsinthebody,arecapableofformingalmostanykindofcellwhentheright"signals"triggertheirdevelopment.
Fortheirtreatmentexperiment,theresearchersreliedonaclassofproteins,bonemorphogenicproteins,thatcauseneuralstem-cell-likeclusterstolosetheirstemcellproperties,whichinturnstopstheirABIlitytodivide.
Firsttheypretreatedhumanglioblastomacellswithbonemorphogenicprotein4(BMP4),theninjectedthesetreatedcellsintomousebrains.Inmiceinjectedwithcellsthatwerenotpretreated,large,invasivecancersgrew.InthemicewithBMP4-treatedcells,nocancersgrewatall.Threetofourmonthsafterinjection,allmicethatgotuntreatedcellsdied,andnearlyallmicewithBMP4-treatedcellswerealive.
Next,thescientistsdeliveredslow-releaseBMP4-containing"beads"directlyintomousebrainswithimplantedglioblastomacells.Micethatgotemptybeadsdevelopedlargemalignanttumorsanddied.MicewithBMP4beadssurvivedmuchlonger,and80percentsurvivedfourmonthsaftercancercellimplants.
"OurideaistotreatpatientswithBMP4orsomethinglikeitrightaftersurgerytoremoveglioblastomainhopesofpreventingtheregrowthofthecancerandimprovingsurvivaltime,"saysAlessandroOlivi,M.D.,directoroftheDivisionofNeurosurgicalOncologyatHopkinsandacontributortothestudy.
OlivisaysclinicalstudiesusingBMP4couldbeginwithinayearand,ifsuccessful,drugtherapiescouldbeavailabletothepublicwithinthreetofouryears.
"ThiswasproofoftheideathatBMPscouldstopglioblastomabydepletingthestem-cell-likepopulationthatfeedsit,"saysHenryBrem,M.D.,chairmanoftheDepartmentofNeurosurgeryatHopkinsandacollaboratorinthestudy."Thisopensexcitingdoorstofutureresearchintotreatmentsandtherapiesforsuchadevastatingdisease."
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