ProductDescription
SP600125isareversIBLeATP-competitive,anthrapyrazolone-basedinhibitorofJNK2andJNK3,withIC50valuesof110and190nM,respectively.Inaselectivitypanel,SP600125was10-foldselecxtiveoverMKK4,25-foldselectiveoverMKK3,MKK6,PKB,andPKCa,and100-foldselectiveforallotherkinasestested.[1]SP600125dose-dependentlyinhibitsphosphorylationfoc-JunandtheexpressionofinflammatorygenesCOX-2(5uM),IL-2(6uM),IFN-g(7uM),andTNF-a(10uM).
IndependentofJNKactivity,SP600125hasbeenshowntopreventtheentryofcellsintomitosisandleadstoendoreplicationofDNAfromtheG2phase.ThisinhibitionpredominantlyoccursupstreamofAIKandPLK1.[2]
SP600125hasalsobeenshowntobealigandandantagoNISTofthearylhydrocarbonreceptor(AhR).Inadose-dependentmanner,SP600125suppressedtheinducdtionofCYP1A1byTCDDandTCDD-inducedAhR-DNAcomplexes.AdditionofSP600125tocytosoljustpriortoTCDDadditioncompletelysuppressesAhRtransformationandDNAbinding(IC50~7uM)[3].
Technicalinformation:
ChemicalFormula: | C14H8N2O | |
CAS#: | 129-56-6 | |
MolecularWeight: | 220.23 | |
Purity: | >98% | |
Appearance: | Yellow | |
ChemicalName: | 2H-Dibenzo[cd,g]indazol-6-one | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | SP600125,SP-600125,Pyrazolanthrone |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Bennettetal.,SP600125,ananthrapyrazoloneinhibitorofJunN-terminalkinase.Proc.Natl.Acad.Sci.,2001,98(24),13681-13686.PubmedID:11717429 |
2. | Kimetal.,SP600125suppressesCdk1andinducesendoreplicationdirectlyfromG2phase,independentofJNKinhibition.Oncogene,2010,29(11),1702-1716.PubmedID:20062077 |
3. | Joiakimetal.,TheJunN-terminalkinaseinhibitorSP600125isaligandandantagonistofthearylhydrocarbonreceptor.DrugMetab.Dispos.2003,31(11),1279-1282.PubmedID:14570754 |
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MaggotsFasterThanScalpelinWoundDebridement
December19,2011—Maggotdebridementtherapy(MDT)appearstobemoreeffectiveforwounddebridementcomparedwithconventionaltherapy,butonlyat1week;afterthattime,anothertypeofdressingshouldbeused,newresearchsuggests.
KristinaOpletalovà,MD,fromtheDepartmentofDermatology,UniversityofCaen,France,andcolleaguespublishedonlineDecember19intheArchivesofDermatology.
MedicalmaggotswereapprovedbytheUSFoodandDrugAdmiNISTrationasamedicaldeviceforwounddebridementin2004.Accordingtotheresearchers,useofmaggotsintreatingwoundsisassociatedwitheffectivewounddebridement,antibacterialeffects,andstimulationofwoundhealing.
However,theypointout,"[r]elativelyfewclinicalstudieshavebeenconductedandtheresultsarenotclear,partlyowingtomethodologicassessmentproblems."
InthecurrentProspective,randomizedcontrolled,phase3clinicaltrial,theresearcherssoughttodeterminetheefficacyofbaggedlarvaeonwounddebridementincomparisonwithconventionaltreatment.
TheprimaryobjectivewastocomparethemeanpercentageofsloughinwoundstreatedwithMDTwiththatofconventionaltreatmentatday15.Thestudyincluded119patientswithanonhealing,sloughywoundthatwas40cm2orsmallerandlessthan2cmdeep.Patientsalsohadananklebrachialindexof0.8orhigher.
Treatmentwasadministeredduringa2-weekhospitalstay.Conventionaltreatmentconsistedofsurgicaldebridement3timesaweekwithascalpel,withuseoftopicalanesthesia.TheMDTwasadministeredusinganencloseddressing(Vitapad,BioMondeLaboratories)containing80sterilemaggots.Atdischarge,aconventionaldressingwasapplied,andpatientswerefollowed-upatday30.
DebridementbyMDTwassignificantlyfasterthansurgicaldebridementduringthefirstweekoftreatment,reachingthesamelevelthecontrolgroupreachedatday15.NobenefitforMDTcomparedwithconventionaltreatmentinhealingrateswasobserved.Atday8,54.5%intheMDTgroupvs66.5%inthecontrolgroup(P=.04)hadevidenceofsloughandwoundhealing.However,byday15,themeanpercentageofsloughwas55.4%intheMDTgroupand53.8%inthecontrolgroup(P=.78).
"AthoughMDTshowsnosignificantbenefitatday15comparedwithconventionaltreatment,debridementbyMDTissignificantlyfasterandoccursduringthefirstweekoftreatment,"theresearchersconclude."Becausethereisnobenefitincontinuingthetreatmentafter1week,anothertypeofdressingshouldbeusedafter2or3applicationsofMDT."
Painscoresweresimilarandmildinbothgroups,althoughincontrasttoconventionaltreatment,MDTwasperformedwithouttopicalanesthesia.
Accordingtotheresearchers,noneofthepatientswerereticentaboutundergoingMDT."[A]crawlingsensationonthewoundwasrarelyandalmostequallynotedinbothgroups,revealingthatthesensationwassubjective,"Dr.Opletalovàandcolleaguespointout.
TwoquestionsregardingMDTremainunanswered,theauthorsnote."Candebridementbeimprovedusingmoremaggotsperdressing?Ifso,wouldthesedressingsbemorepainful?Furtherstudiesareneededtoanswerthesequestions."
ThestudywassupportedbygrantsfromtheClinicalResearchHospitalProgramandfromtheFrenchSocietyofDermatology.Theauthorshavedisclosednorelevantfinancialrelationships.
1. 姜黄素是一个典型的HAT抑制剂。
2. 针对P300: 在大约10年前,Cole和他的同事设计出了一种p300/CBP抑制剂,发表在nature杂志上。
希望能帮到你,望采纳!
天然产物,大多都有颜色,
存在干扰,多数情况下需要做样品的阴性对照,
尽量能用荧光的方法,
之前我们做过,将两个试剂盒的方法合并后,做的,
效果还可以
支原体培养则是取样后在培养基上培养,看有多少支原体菌落会长出,是比较直观和可信的结果。
总体来讲,这两种检查手段可信度都较高,结合一起,不仅可以可靠的知道有无解脲支原体感染,还能知道感染是否严重。
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