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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDeferoxamineCat.No.:HY-B1625CASNo.:70-51-9Synonyms:DeferoxamineB;DeferriferrioxamineB;Deferrioxamine分?式:C??H??N?O?分?量:560.68作?靶點:HIF/HIFProlyl-Hydroxylase;ReactiveOxygenSpecies;Apoptosis;Akt;Autophagy作?通路:MetabolicEnzyme/Protease;Immunology/Inflammation;NF-κB;Apoptosis;PI3K/Akt/mTOR;Autophagy儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Deferoxamine(DeferoxamineB)?種鐵螯合劑(結合Fe(III)和許多其他?屬陽離?),被?泛?于減少鐵在組織中的積累和沉積。Deferoxamine具有較好的抗氧化活性,可上調HIF-1α?平。Deferoxamine還具有抗增殖活性,能誘導癌細胞凋亡和?噬。Deferoxamine可?于糖尿病、神經(jīng)退?性疾病以及抗癌和抗COVID-19的研究。體外研究Deferoxamine(1mM;16hor4weeks)improvesHIF-1αfunctionunderhypoxicandhyperglycemicconditionsanddecreasesROSinMEFscells[1].Deferoxamine(100μM;24h)increasesInsRexpressionandactivityandalsoinducesanincreaseinp-Akt/totalAkt/PKBlevels[2].Deferoxamine(5,10,25,50,100μM;7or9days)inhibitstheproliferationoftumor-associatedMSCsandbonemarrowMSCs[3].Deferoxamine(5,10,25,50,100μM;7days)inducesapoptosisofMSCs[3].Deferoxamine(10μM;3days)influencstheexpressionofadhesionproteinsonMSCs[3].Deferoxamine(100μM;24h)inducesautophagymediatedbythelevelofHIF-1αinSH-SY5Ycells[4].WesternBlotAnalysis[1]CellLine:MEFscellsConcentration:1mM1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:16h(hypoxiacondition);4weeks(hyperglycemicconditions)Result:Significantlyattenuatedthehyperglycemia-associatedincreaseinROSlevelsunderhypoxichighglucoseconditions.NotablyincreasednormoxicHIFtransactivationinMEFsunderbothhighglucoseandnormalglucoseconditions.WesternBlotAnalysis[2]CellLine:HepG2cellsConcentration:100μMIncubationTime:24hResult:ShowedatwofoldincreaseofInsRmRNAlevelsincells.IncreasedbytwofoldInsRbindingactivityatthehalf-maximalconcentrationof1.1nM.CellProliferationAssay[3]CellLine:TAMSCsandBMMSCs(allisolatedfromMaleC57BL/6Jmice(8week-old;EG-7inducedtumormodel))Concentration:5,10,25,50,100μMIncubationTime:7days(TAMSCs);9days(BMMSCs).Result:InhibitedthegrowthofTAMSCsandBMMSCs,andmostcellsarediedatday7or9whenexposedto50and100μMdose.ApoptosisAnalysis[3]CellLine:TAMSCs,BMMSCsConcentration:5,10,25,50,100μMIncubationTime:7daysResult:ExhibitedproapoptoticeffectonTAMSCsandBMMSCscells.WesternBlotAnalysis[3]CellLine:TAMSCs,BMMSCsConcentration:10μMIncubationTime:3daysResult:RemarkablydecreasedVCAM-1expressioninbothTAMSCsandBMMSCs.2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellAutophagyAssay[4]CellLine:SH-SY5YcellsConcentration:100μMIncubationTime:24hResult:IncreasedtheratioofLC3-II/I,anindicatorofautophagy,whicheffectswereblockedwhenautophagy-relatedgeneBeclin1wassuppressedbyBeclin1siRNAtransfection.Causedatimeanddose-dependentincreaseofHIF-1a,accompaniedbytheinductionofautophagy.體內(nèi)研究Deferoxamine(560.68mg/per;drip-on;oncedailyfor21days)enhanceswoundhealingandincreasesneovascularizationinagedordiabeticmice[1].Deferoxamine(200mg/kg;i.p.;dailyfor2weeks)resultsinHIF-1αstabilizationandincreasesglucoseuptake,hepaticInsRexpression,andsignalinginvivo[2].AnimalModel:Aged(21-month-old)anddiabetic(12-week-old)C57BL/6Jmice(excisionalwoundmodel)[1].Dosage:560.68mg/per(10uLof1mM)Administration:Drip-on;oncedailyfor21days.Result:Displayedsignificantlyacceleratedhealingandincreasedneovascularizationinbothagedanddiabeticmicemodel.AnimalModel:MaleSprague-Dawleyrats(180-200g)[2].Dosage:200mg/kgAdministration:Intraperitonealinjection;dailyfor2weeks.Result:SignificantlyincreasedhepaticHIF-1αproteinlevels,InsRproteinlevels,aswellasAkt/PKBandactivatedAkt/PKBweresignificantlyhigherintheliver.戶使?本產(chǎn)品發(fā)表的科研?獻?SignalTransductTargetTher.2020May8;5(1):51.?CellRes.2018Dec;28(12):1171-1185.?AdvSci(Weinh).2021Mar8;8(10):2004680.?BioactMater.19November2021.?SciAdv.2022Mar4;8(9):eabm1896.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].DuscherD,etal.ComparisonoftheHydroxylaseInhibitorDimethyloxalylglycineandtheIronChelatorDeferoxamineinDiabeticandAgedWoundHealing.PlastReconstrSurg.2017Mar;139(3):695e-706e.[2].DongiovanniP,etal.Irondepletionbydeferoxamineup-regulatesglucoseuptakeandinsulinsignalinginhepatomacellsandinratliver.AmJPathol.2008Mar;172(3):738-47.[3].WangG,etal.Invitroassessmentofdeferoxamineonmesenchymalstromalcellsfromtumorandbonemarrow.EnvironToxicolPharmacol.2017Jan;49:58-64.[4].WuY,etal.Neuroprotectionofdeferoxamineonrotenone-inducedinjuryviaaccumulationofHIF-1alphaandinductionofautophagyinSH-SY5Ycells.NeurochemInt.2010Oct;57(3):198-205.[5].BellottiD,etal.DeferoxamineB:ANatural,ExcellentandVersatile
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