Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemECZL-S092Cat.No.:HY-176734分子式:C??H??FN?OS分子量:418.49作用靶點(diǎn):Polo-likeKinase(PLK)作用通路:CellCycle/DNADamage儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CZL-S092(Compound34b)是一種PLK4抑制劑，對(duì)其他PLK4家族成員(PLK1、PLK2和PLK3)具有極高的選擇性，其IC50為0.9nM。CZL-S092在體外表現(xiàn)出抗神經(jīng)母細(xì)胞瘤活性(IMR-32,IC50=1.143μM)。CZL-S092可抑制細(xì)胞遷移，阻滯細(xì)胞周期，誘導(dǎo)細(xì)胞凋亡(apoptosis)。CZL-S092可用于神經(jīng)母細(xì)胞瘤等多種癌癥研究[1]。IC50&TargetPLK40.9nM(IC50)體外研究CZL-S092(0.5μM;60min)inhibitsPLK4by>80%inapanelof37kinasesandexhibitsexcellentselectivityoverotherPLKfamilymembers(PLK1,PLK2,andPLK3)[1].CZL-S092(0.5-2.5μM,5d)exhibitstheoptimalantiproliferativeactivityagainstMCF-7,IMR-32andSH-SY5YcellswithIC50valuesof2.828μM,1.143μM,and1.329μM,respectively[1].CZL-S092(0.5-5μM;48h)inducessignificantapoptosis(84.3%)inIMR-32neuroblastomacells[1].CZL-S092(2.5μM;48h)arrestesIMR-32cellsatG2/Mphase(87.4%)[1].CZL-S092(5.0μM;24h)significantlysuppressesIMR-32cellmigration(>90%)[1].CellProliferationAssay[1]CellLine:MCF-7,IMR-32,SH-SY5YConcentration:0.5μM,1.0μM,2.5μMIncubationTime:5daysResult:ExhibitedtheoptimalantiproliferativeactivityagainstMCF-7,IMR-32andSH-SY5Ycells1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEwithIC50valuesof2.828μM,1.143μM,and1.329μM,respectively.CellCycleAnalysis[1]CellLine:IMR-32Concentration:1.0μM,2.5μM,5.0μMIncubationTime:48hResult:Producedaremarkable87.4%and89.6%G2/Mphasearrestataconcentrationof2.5μMand5.0μM.ApoptosisAnalysis[1]CellLine:IMR-32Concentration:1.0μM,2.5μM,5.0μMIncubationTime:48hResult:Inducedthetotalrateto84.3%ataconcentrationof2.50μM,and90.2%at5.0μM.CellMigrationAssay[1]CellLine:IMR-32Concentration:1.0μM,2.5μM,5.0μMIncubationTime:24hResult:Significantlysuppressedover90%ofthewoundhealingwith5.0μM.Immunofluorescence[1]CellLine:IMR-32Concentration:2.5μMIncubationTime:48hResult:Occurreddisorderedcentrosomereplicationandresultedincentrioleloss.T.REFERENCESLiuNetal.RationaldesignofCZL-S092:Anovelindazole-basedPLK4inhibitortargetingneuroblastomathroughvirtualscreeningandfragment-baseddrugdesignstrategies.EurJMedChem.2025Jun13;296:117867.doi:10.1016McePdfHeight2/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.For