Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENovobiocinCat.No.:HY-B0425CASNo.:303-81-1Synonyms:Albamycin;Cathomycin分?式:C??H??N?O??分?量:612.62作?靶點(diǎn):Antibiotic;DNA/RNASynthesis;HSP;Apoptosis;Bacterial;Orthopoxvirus作?通路:Anti-infection;CellCycle/DNADamage;MetabolicEnzyme/Protease;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Novobiocin(Albamycin)?種有效且具有?服活性的抗?素。Novobiocin還DNA促旋酶抑制劑和熱休克蛋?90(Hsp90)拮抗劑。Novobiocin具有研究?度耐藥性肺炎球感染的潛?.Novobiocin具有抗正痘活性[1][2][3][4]。IC50&TargetHSP90體外研究Novobiocin(1mM)competitivelyinhibitsATPbindingtogyraseBtointerferewithnucleotidebindingandinterfereswiththeassociationoftheco-chaperonesHsc70andp23withHsp90[1].Novobiocin(200μM;24h)inhibitstherateofrepairofbothcis-DDPandBCNUinducedDNAinterstrandcross-linksandwithacorrespondingdecreaseintheclonogenicsurvivalofthehumanglioblastomamultiformecells[2].Novobiocin(0.3mM;48hours)inducesacaspase-3/7enzyme–dependentapoptosisassayswithaninductionofapproximatelythree-tofivefoldofapoptoticcellsinK562,HL60,Mutz-2[5].體內(nèi)研究Novobiocin(25,50,100,200mg/kg;s.c.;4timesat1,5,24and48hafterinfection)showsanti-infectionactivityinmiceinfectedwithamoxicillin-resistantStreptococcuspneumoniae[3].AnimalModel:30gadultfemaleSwissmice(sepsisinducedbythepenicillin-susceptiblestrain(AR33118))[3]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:25,50,100,200mg/kgAdministration:S.c.;givenat1,5,24and48hafterinfectionResult:Showedanti-infectionactivityinmiceinfectedwithamoxicillin-resistantS.pneumoniae.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Blood.2018Jul19;132(3):307-320.?IntJMolSci.2019Mar5;20(5).pii:E1125.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MarcuMG,etal.Theheatshockprotein90antagonistnovobiocininteractswithapreviouslyunrecognizedATP-bindingdomaininthecarboxylterminusofthechaperone.JBiolChem.2000Nov24;275(47):37181-6.[2].Ali-OsmanF,etal.TopoisomeraseIIinhibitionandalteredkineticsofformationandrepairofnitrosoureaandcisplatin-inducedDNAinterstrandcross-linksandcytotoxicityinhumanglioblastomacells.CancerRes.1993Dec1;53(23):5663-8.[3].Rodríguez-CerratoV,etal.Comparativeefficacyofnovobiocinandamoxicillininexperimentalsepsiscausedbybeta-lactam-susceptibleandhighlyresistantpneumococci.IntJAntimicrobAgents.2010Jun;35(6):544-9.[4].EderJP,etal.AphaseIclinicaltrialofnovobiocin,amodulatorofalkylatingagentcytotoxicity.CancerRes.1991Jan15;51(2):510-3.[5].BhatiaS,etal.TargetingHSP90dimerizationviatheCterminusiseffectiveinimatinib-resistantCMLandlackstheheatshockresponse.Blood.2018Jul19;132(3):307-320.[6].SmeeDF.Progressinthediscoveryofcompoundsinhibitingorthopoxvirusesinanimalmodels.AntivirChemChemother.2008;19(3):115-24.[7].SmeeDF.Progressinthediscoveryofcompoundsinhibitingorthopoxvirusesinanimalmodels.AntivirChemChemother.2008;19(3):115-24.McePdfHeightCaution:Producthasnotbeenfullyva