Sertaconazole-FI7056-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESertaconazoleCat.No.:HY-B0736CASNo.:99592-32-2Synonyms:FI7056freebase分?式:C??H??Cl?N?OS分?量:437.77作?靶點(diǎn):Fungal;Autophagy;Apoptosis;p38MAPK;Microtubule/Tubulin作?通路:Anti-infection;Autophagy;Apoptosis;MAPK/ERKPathway;CellCycle/DNADamage;Cytoskeleton儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Sertaconazole(FI7056freebase)?種局部?譜的抗真劑，可通過(guò)激活p38-COX-2-PGE2通路來(lái)發(fā)揮抗炎活性。Sertaconazole也?種微管蛋?抑制劑，具有抗癌細(xì)胞增殖活性，誘導(dǎo)細(xì)胞的凋亡和?噬，還能抑制細(xì)胞的遷移，具有較好的抗癌活性。體外研究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?邊的抑制劑?師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?邊的抑制劑?師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?邊的抑制劑?師www.MedChemEautophagyinA549andH460cells.體內(nèi)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.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MedComm.16December2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Carrillo-Mu?ozAJ,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