GIC-20-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEGIC-20Cat.No.:HY-162449CASNo.:2942242-60-4分子式:C₃₈H₃₇ClN₄O₅S分子量:697.24作用靶点:Apoptosis;Ferroptosis作用通路:Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性GIC-20是细胞凋亡(apoptosis)和铁死亡(ferroptosis)的双重诱导剂。GIC-20对纤维肉瘤具有抗肿瘤活性[1]。体外研究GIC-20(1μM,48h)inhibitsproliferationandmigrationofHT1080fibrosarcomacells,exhibitscytotoxicitywithIC50of1.6μM[1].GIC-20(0.5-4μM,24h)inducesferroptosisbyinducingintracellularlipidperoxideandROSaccumulation,orbydegradationofGPX4[1].GIC-20(0-1μM,24h)inhibitscellviabilityofdrug-resistantMIA-PaCa-2-AMG510Rcells,enhancesthesensitivityofMIA-PaCa-2-AMG510RcellstoAMG510[1].WesternBlotAnalysis[1]CellLine:HT1080Concentration:0-4μMIncubationTime:24hResult:InhibitedexpressionofGPX4andBcl-2,promotedexpressionofBax.ApoptosisAnalysis[1]CellLine:HT1080Concentration:0-4μM1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:24hResult:Inducedapoptosisinadose-dependentmanner.体内研究GIC-20(20-40mg/kg,i.p.,oncedailyfor19days)exhibitsantitumorefficacyinHT1080xenograftBALB/cmice,withoutsignificanttoxicityinmajororgans[1].AnimalModel:HT1080xenograftBALB/cmice[1]Dosage:20-40mg/kgAdministration:i.p.,onceadayfor19daysResult:Inhibitedtumorgrowth,withaTGIof63%at40mg/kg.Maintainedacompletemorphologywithoutobviouscellularinflammatory,oedema,ornecrosisinmajororgans.REFERENCESMaF,etal.,ML162derivativesincorporatinganaphthoquinoneunitasferroptosis/apoptosisinducers:Design,synthesis,anti-canceractivity,anddrug-resistancereversalevaluation.EurJMedChem.2024Apr15;270:116387.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3