PRDX1-IN-1-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPRDX1-IN-1Cat.No.:HY-149394分子式: C??H??N?O?分子量: 713.95作用靶點(diǎn): Others;ROSKinase;Apoptosis作用通路: Others;ProteinTyrosineKinase/RTK;Apoptosis儲存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PRDX1-IN-1是PRDX1的選擇性抑制劑，IC50值為0.164μM。PRDX1-IN-1可用于癌癥相關(guān)研究。PRDX1-IN-1促進(jìn)細(xì)胞內(nèi)ROS積累，除誘導(dǎo)細(xì)胞凋亡外，還抑制癌細(xì)胞的增殖、侵襲和遷移。PRDX1-IN-1可用于癌癥研究[1]。IC50&TargetIC50:0.164μM(potentperoxiredoxin1,PRDX1)[1]體外研究PRDX1-IN-1inhibitestheproliferationactivitiesofthehumanlungcancercellsA549,lungcancercelllines(LTEP-a-2andH1975),humanbreastcancercellline(MDA-MB-231),humanhepatomacellline(SK-Hep-1)withtheIC50valuesof1.92μM，2.93μM，1.99μM，2.67μM，2.42μM，respectively[1].PRDX1-IN-1(compound7e)(2μMor4μM,24h)promotesintracellularROSaccumulation,andinhibitstheinvasionandmigrationofhumanlungcancercellsA549[1].PRDX1-IN-1(2μMor4μM,24h)inducestheapoptosisofA549cells[1].PRDX1-IN-1(2μMor4μM,6h)suppressesthekeysignalingpathways(AKTandERK)andpromotestheexpressionofapoptosis-relatedproteins(cleavedcaspase-3/8andcleavedPARP)inA549cells[1].Proliferationassay[1]CellLine:lungcancercelllines(LTEP-a-2andH1975),humanbreastcancercellline(MDA-MB-231),humanhepatomacellline(SK-Hep-1)Concentration:0.5–10μMIncubationTime:48hResult:InhibitedtheproliferationactivitiesofcancercellsA549,LTEP-a-2,H1975,MDA-MB-1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE231,SK-Hep-1.Apoptosisassay[1]CellLine:humanlungcancercellsA549Concentration:2μMor4μMIncubationTime:24hResult:Increasedtheratioofthetotalnumberofearly(annexin-V+/PI?)andlate(annexin-V+/PI+)apoptoticcellssignificantly.WBassay[1]CellLine:A549cellConcentration:2μMor4μMIncubationTime:6hResult:DecreasedthephosphorylationlevelsofPI3K,AKT,C-RAFandERK.Matrigelinvasionassay[1]CellLine:A549cellConcentration:2μMor4μMIncubationTime:24-48hResult:Inhibtedthecellmatrigelandinvasion.體內(nèi)研究PRDX1-IN-1(0.5or1mg/kg,intraperitoneal(i.p.),19days,everyday)inhibitedtumorgrowthinamousemodeloflungcancer[1].AnimalModel:C57BL/6JmalemiceinjectedwithLewiscell(lungcancer)[1]Dosage:0.5or1mg/kgAdministration:intraperitonealinjection(i.p.),everydayfor19days.Result:Inhibitedtumorgrowth,withthetumorgrowthinhibition(TGI)valuesof77.47%and69.89%inthegroupsof1mg/kgand0.5mg/kg,respectively.Inducedthechangesinmorphologicalcharacteristicsoftumorcells,includingcellagglutination,contraction,andnuclearchromatinmarginalization.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEYingBai,etal.Developmentofnovelcelastrol-ligustrazinehybridsaspotentperoxiredoxin1inhibitorsagainstlungcancer.EurJMedChem.2023,259,115656.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor