Sertaconazole-FI7056-free-base-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESertaconazoleCat.No.:HY-B0736CASNo.:99592-32-2Synonyms:FI7056freebase分⼦式:C₂₀H₁₅Cl₃N₂OS分⼦量:437.77作⽤靶点:Fungal;Autophagy;Apoptosis;p38MAPK;Microtubule/Tubulin作⽤通路:Anti-infection;Autophagy;Apoptosis;MAPK/ERKPathway;CellCycle/DNADamage;Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Sertaconazole(FI7056freebase)⼀种局部⼴谱的抗真剂，可通过激活p38-COX-2-PGE2通路来发挥抗炎活性。Sertaconazole也⼀种微管蛋⽩抑制剂，具有抗癌细胞增殖活性，诱导细胞的凋亡和⾃噬，还能抑制细胞的迁移，具有较好的抗癌活性。体外研究Sertaconazole(0.03-40µg/mL;24h)inhibits150strainsofyeastswhichincludessixCandidaspecieswitharithmeticmeanMICof0.77µg/mL[1].Sertaconazole(1µg/mL;5,10,30,60min)activatesp38MAPkinaseinatime-dependentmanner[2].Sertaconazole(1,2µg/mL;6,8,or24h)increasesatwofoldreleaseofPGE2viaCOX-2inkeratinocytes,whichisdependentonp38activation[2].Cetaconazole(10,20,30,40µM;24h)inducesstrongmitoticarrestbydepolymerizinginterphaseandspindlemicrotubules,therebyinducingchromosomeaggregationdefectsandcausinganti-proliferationeffect[3].Sertaconazole(20,40µM;24h)inducesapoptosisthroughp53pathwayinHeLacells[3].Sertaconazole(20,30µM;24,48,and72h)inhibitsthemigrationofHeLacellsinaconcentration-dependentmanner[3].Sertaconazole(15,30µM;24h)inducesautophagyinA549,H460cells[4].CellViabilityAssay[1]CellLine:C.albicans,C.guilliermondii,C.krusei,C.parapsilosi,C.tropicalis,C.glabrata1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:0.03-40µg/mIncubationTime:24hResult:Againsted150strainsofyeasts(sixCandidaspecies)whichincludedC.albicans,C.guilliermondii,C.krusei,C.parapsilosi,C.tropicalis,C.glabrataspecieswitharithmeticmeanMICvaluesof1.02,0.51,0.38,0.31,1.67and0.78µg/mL,respectively.WesternBlotAnalysis[2]CellLine:HaCaTcellsConcentration:1µg/mLIncubationTime:5,10,30,60minResult:Showedactivityofactivatingp38MAPkinaseandHsp27inatime-dependentmanner.WesternBlotAnalysis[2]CellLine:HaCaTcellsConcentration:1,2µg/mLIncubationTime:6or8hResult:Induced50%expressionofCOX-2andresultedinatwofoldincreasedinPGE2release.WesternBlotAnalysis[2]CellLine:siRNA-transfectedHaCaTcells(withoutp38MAPkinaseexpression)Concentration:1µg/mLIncubationTime:24hResult:MediatedinductionofPGE2wasdependentonp38activation.CellProliferationAssay[3]CellLine:HeLa,HEK-293,MCF-7,A549cellsConcentration:0-100µMIncubationTime:24hResult:ShowedantiproliferationactivitywithIC50sof38,45.1,41.5,and40.8μMforHeLa,HEK-293,A549,andMCF-7cells,respectively.Exhibitedmitoticblockactivityandinducedcelldeathatconcentrationabove30μM,but2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEnosignificantincreasedinthenumberofmitoticcells.Depolymerizedinterphaseandspindlemicrotubulesinducingdefectinchromosomalcongression.ApoptosisAnalysis[3]CellLine:HeLacellsConcentration:10,20,40µMIncubationTime:24hResult:Inducedapproximately5%,10%,and21%cellsapoptoticatconcentrationsof10,20and40μM,respectively.WesternBlotAnalysis[3]CellLine:A549cellsConcentration:20,40µMIncubationTime:24hResult:Inducedapoptosisthroughp53pathwaythattheexpressionofp53from30%to50%and95%andp21from11to39%and40%respectively.ResultedinNoxaandPuma,twodirecttranscriptionaltargetsofp53tobeoverexpressed.CellMigrationAssay[3]CellLine:HeLacellsConcentration:20,30µMIncubationTime:24,48,and72hResult:InhibitedthemigrationofHeLacellsatconcentrationslesserthanitsIC50,whichinaconcentration-dependentmanner.CellAutophagyAssay[4]CellLine:A549,H460cellsConcentration:15,30µMIncubationTime:24hResult:IncreasedendogenousLC3punctaandLC3intensity,whichindicatedinductionof3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEautophagyinA549andH460cells.体内研究Sertaconazole(1%(w/v);applytotheleftear,once)suppressesofTPA-inducedearedemaCD-1mice[2].AnimalModel:CD-1mice(TPA-inducedearedemamodel)[2].Dosage:1%(w/v)Administration:Applytotheleftear,once.Result:ExhibitedasignificantreductionofinflammationinmicebymediatingPGE2release.户使⽤本产品发表的科研⽂献•MedComm.16December2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Carrillo-MuñozAJ,etal.In-vitroantifungalactivityofsertaconazole,econazole,andbifonazoleagainstCandidaspp.JAntimicrobChemother.1995Oct;36(4):713-6.[2].SurR,etal.Anti-inflammatoryactivityofsertaconazolenitrateismediatedviaactivationofap38-COX-2-PGE2pathway.JInvestDermatol.2008Feb;128(2):336-44.[3].SebastianJ,etal.SertaconazoleinducedtoxicityinHeLacellsthroughmitoticarrestandinhibitionofmicrotubuleassembly.NaunynSchmiedebergsArchPharmacol.2021Jun;394(6):1231-1249.[4].ZhangW,etal.SertaconazoleprovokesproapoptoticautophagyviastabilizingTRADDinnonsmallcelllungc