Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE5-AminosalicylicAcidCat.No.:HY-15027CASNo.:89-57-6Synonyms:Mesalamine;5-ASA;Mesalazine分?式:C?H?NO?分?量:153.14作?靶點:PPAR;PAK;NF-κB;EndogenousMetabolite作?通路:CellCycle/DNADamage;Cytoskeleton;NF-κB;MetabolicEnzyme/Protease儲存?式:4°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數據體外實驗DMSO:≥6mg/mL(39.18mM)H2O:2mg/mL(13.06mM;ultrasonicandwarmingandheatto60°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM6.5300mL32.6499mL65.2997mL5mM1.3060mL6.5300mL13.0599mL10mM0.6530mL3.2650mL6.5300mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：50%PEG300>>50%salineSolubility:7.14mg/mL(46.62mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：PBSSolubility:1.43mg/mL(9.34mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性5-Aminosalicylicacid(Mesalamine)?種特異性的PPARγ激動劑，還抑制p21-激活激酶1(PAK1)和NF-κB。IC50&TargetPPARγPAK1p65體外研究5-Aminosalicylicacid(5-ASA)isaspecificagonistforPPARγ,andonlyPPARγbutnotPPARαorPPARδinducesp65degradation.5-Aminosalicylicacidinducesdegradationofp65proteinindicativeofPPARγ'sE3ubiquitinligaseactivity.5-AminosalicylicacidalsoinhibitsPAK1atthemRNAlevelwhichissuggestiveofanadditionalmechanismindependentofPPARγligandactivation.5-AminosalicylicacidblocksNF-κBinintestinalepithelialcells(IECs)throughinhibitionofPAK1[1].Pretreatmentwith5-Aminosalicylicacid(5-ASA)orNimesulideatdifferentconcentration(10-1000μmol/L)for12-96h,inhibitsthegrowthofHT-29coloncarcinomacellsinadoseandtime-dependentmanner.However,thesuppressionof5-AminosalicylicacidorNimesulidehasnostatisticalsignificance.ThegrowthofHT-29coloncarcinomacellsisinhibiteddose-dependentlywhenpretreatedwithdifferentdosesofcombined5-AminosalicylicacidandNimesulide.Combined5-Aminosalicylicacid(finalconcentration100μM)andNimesulide(finalconcentration10-1000μM)inhibitstheproliferationofHT-29coloncarcinomacellsinadose-dependentmanner,beingmorepotentthancorrespondingdoseofNimesulide.Similarly,combinedNimesulide(finalconcentration100μM)and5-Aminosalicylicacid(finalconcentration10-1000μM)alsoinhibitstheproliferationofthesecellsdose-dependently,beingmorepotentthancorrespondingdoseof5-Aminosalicylicacid[2].體內研究5-Aminosalicylicacid(5-ASA)hasanantineoplasticeffectinaxenografttumormodel.Toevaluatetheinvivoantineoplasiceffectof5-Aminosalicylicacid,SCIDmiceengraftedwithHT-29coloncancercellsaretreateddailyfor21consecutivedayswith5-Aminosalicylicacidat50mM.Attheendofthetreatment,areductionof80-86%oftumorweightandvolumeisobservedinSCIDmicereceiving5-AminosalicylicacidcomparedwithcontrolmiceormicetreatedwithGW9662alone.Theantineoplasticeffectof5-Aminosalicylicacidisalreadydetectableafter10daysof5-Aminosalicylicacidtreatment.Similarresultsareobtainedwithmicetreatedwith5-Aminosalicylicacidat5mM.Antitumorigeniceffectof5-Aminosalicylicacidiscompletelyabolishedat21daysbysimultaneousintraperitonealadministrationofGW9662.Thus,theobservedantineoplasticeffectof5-AminosalicylicacidisatleastpartiallydependentonPPARγ[3].PROTOCOLCellAssay[2]CytostaticeffectsaremeasuredbyMTTassay.HT-29coloncarcinomacellsaredetachedwitha0.25%trypsinsolutionfor5min.Subsequently,thecellsareseededonto96-wellplates(1×106cells/well),supplementedwith10%FCSandallowedtoattachfor24hbeforetheadditionoftestcompounds(5-2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAminosalicylicacid10,50,100,500,and1000μM;Nimesulide;andtheircombination).Testcompoundsaredilutedinserum-freeculturemedium.Thenthecellsareincubatedinamediumoratdifferentconcentrationsofdrugsfor48h,20μLofMTTsolution(5g/L)inPBSisadded.Fourhourslater,themediumineachwellisremoved,and120μLof0.04mMmuriaticisopropanolisadded,slightlyconcussedfor10min.Dyeuptakeismeasuredat490nmwithanELISAreader.Fivewellsareusedforeachconcentrationorasacontrolgroup.Ontheotherhand,thecellsareseededonto96-wellplates(1×106cells/well)andallowedtoattachfor24h,thentreatedwithtestcompounds(5-Aminosalicylicacid,Nimesulide,andtheircombination).Thefinalconcentrationis100μM.Thesamemediumisaddedintothecontrolgroupanddyeuptakeisthenmeasured.Fivewellsareusedforeachtestcompoundorcontrolgroup[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[3]Administration[3]Sixtosevenweeksoldpathogen-freeBALB/cSCIDmiceareused.Humancoloncancercells(107HT-29cells)pretreatedornotwithGW9662for24hareimplantedsubcutaneouslyintheflankofanimals.Twodaysaftercellinoculation,micearetreatedwith5-Aminosalicylicacid(5or50mM)administereddailybyperitumoralinjectionfor10or21days.TheeffectofPPARγduring5-AminosalicylicacidtreatmentisevaluatedbydailyintraperitonealinjectionofGW9662(1mg/kg/day).Thecontrolgroupreceivessalineinsteadof5-Aminosalicylicacid.Micearecheckedthreetimesaweekfortumordevelopment.Afterkillingat10or21days,tumorsizeandvolumearecalculated.Tumorsareweightedbeforeparaffinembeddingforhistologicalexamination.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?BrainBehavImmun.2020Nov;90:108-137.?CarbohydrPolym.2022:120329.?Phytomedicine.November2022,154438.?Phytomedicine.2022Jan29;98:153961.?BiochemPharmacol.2021Jun4;190:114645.SeemorecustomervalidationsonHYPERLINK"