JH530-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEJH530Cat.No.:HY-149847分子式: C₂₂H₂₄BrN₇O₂S分子量: 530.44作用靶点: Others作用通路: Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性JH530是一种有效的巨泡式细胞死亡(methuosis)诱导剂，通过引起细胞内完全空泡化来抑制三阴性乳腺癌(TNBC)细胞的增殖。JH530具有抗肿瘤活性，可用于癌症研究。IC50&TargetMethuosis[1]体外研究JH530(compound5c)(1μMor2μM;24hours)causesnotablecellularmorphologicalchangesinHCC1806cells,characterizedbytheaccumulationofintracellularvacuoles,andscarcelyaffectedthemorphologyof184B5cellsandcellviability[1].JH530(0.5,1.0,1.5μM;24hours)causescelldeathbymethuosis[1].JH530(1μM;24hours)effectivelysuppressestheproliferationofTNBCcellsinvitro[1].JH530(1.5μM;24hours)causestheincreaseofRab7andLamp1expressioninHCC1806andMDA-MB-468[1].CellProliferationAssay[1]CellLine:HCC1806,HCC1937,MDA-MB-468cellsConcentration:1μMIncubationTime:24hoursResult:Expressedremarkableanti-proliferativeactivitiesinvitro,withtheIC50valueswere0.70μM,0.92μM,and1.03μMforthreeTNBCcellsHCC1806,MDA-MB-468,andHCC1937,respectively.CellViabilityAssay[1]1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellLine:HCC1806,184B5Concentration:1μMor2μMIncubationTime:24hoursResult:Exhibitednotablecellularmorphologicalchangesat1μM,characterizedbytheaccumulationofintracellularvacuolesinHCC1806cells.Scarcelyaffectedthemorphologyof184B5cellsandcellviability.WesternBlotAnalysis[1]CellLine:HCC1806;MDA-MB-468Concentration:0,0.5,1.0,1.5μMIncubationTime:24hoursResult:Dose-dependentlyinducedtheincreaseofRab7andLamp1expression,andcausescelldeathbymethuosis.Immunofluorescence[1]CellLine:HCC1806,HCC1937,MDA-MB-468cellsConcentration:1.5μMIncubationTime:24hoursResult:InducedtheincreaseofRab7andLamp1expressioninHCC1806andMDA-MB-468.Inducedtheaccumulationofvacuolesinmostofthecell.体内研究JH530(compound5c)(2.5mg/kgor5.0mg/kg;i.p.;onceevery2daysfortwoweek)elicitestumorregressionandwelltoleratedwithtreatmentdoseswithoutcausinganoticeableweightdecrease[1].AnimalModel:HCC1806cellxenograftmousemodel[1]Dosage:2.5mg/kg,5.0mg/kgAdministration:Intraperitonealinjection(i.p.);onceevery2daysResult:InhibitsHCC1806tumorweightat2.5mg/kgsignificantly,whileexhibitmoreapparenttumorsuppressiveeffectsat5mg/kg[1].REFERENCES2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEHeJ,etal.DiscoveryofPyrimidinediamineDerivativesasPotentMethuosisInducersfortheTreatmentofTriple-NegativeBreastCancer.JMedChem.2023Jun8;66(11):7421-7437.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp