ZWZH-21-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEZWZH-21Cat.No.:HY-175513CASNo.:3069195-42-9分子式:C₂₆H₂₂N₄O₂分子量:422.48作用靶点:HDAC;Apoptosis作用通路:CellCycle/DNADamage;Epigenetics;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性WZH-21是一种选择性且具有口服活性的HDAC1/2双重抑制剂，对HDAC1的IC50值为34nM，对HDAC2的值为41nM。ZWZH-21能够抑制HCT116和SW480细胞的生长，IC50值分别为0.524μM和1.063μM。ZWZH-21可以抑制多种结直肠癌细胞的增殖和迁移，并诱导其凋亡(apoptosis)。ZWZH-21可用于癌症研究，如结直肠癌研究[1]。IC50&TargetHDAC1HDAC2HDAC3HDAC634nM(IC50)41nM(IC50)277nM(IC50)>800nM(IC50)HDAC8>800(IC50)体外研究ZWZH-21inhibitsA549,MCF-7andHepG2cellsgrowthwithIC50valuesof1.66μM,2.445and1.551μM,respectively[1].ZWZH-21(1μM,6h)inhibitstemperature-inducedHDAC1/2degradationinHCT116cells[1].ZWZH-21(0.4-1.6μM,48h)inducesthedegradationofHDAC1andHDAC2proteinandtheformationofAc–H3andhistoneH4inaconcentration-dependentmannerinHCT116cells[1].ZWZH-21(0.4-1.6μM,48h)inhibitsthecolony-formingabilityinHCT116andSW480cells[1].ZWZH-21(0.4-2μM,48h)suppressescellmigrationandinducesapoptosisinHCT116andSW480cells[1].ZWZH-21(0.4-2μM,24h)inducesG1phasearrestinHCT116andSW480cells[1].WesternBlotAnalysis[1]CellLine:HCT116cells1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:0.4,0.8,and1.6μMIncubationTime:48hResult:ReducedHDAC1andHDAC2proteinandincreasedAc–H3andAc–H4levels.ApoptosisAnalysis[1]CellLine:HCT116cellsandSW480cellsConcentration:0.4,0.8and1.6μMinHCT116,0.5,1and2μMinSW480cellsIncubationTime:48hResult:SignificantlyincreasedtheproportionofAnnexinV-positivecells.Showedhighestapoptoticratesreaching60.7%and40.04%atlowconcentrations.CellCycleAnalysis[1]CellLine:HCT116cellsandSW480cellsConcentration:0.4,0.8and1.6μMinHCT116,0.5,1and2μMinSW480cellsIncubationTime:24hResult:Demonstratedadose-dependentaccumulationofcellsinG1phase.体内研究ZWZH-21(2000mg/kg,orallyonce)showsagoodsafetyinmice[1].ZWZH-21(30-120mg/kg,i.g.,dailyfor14days)suppressestumorgrowthinmicebearingHCT116humancoloncancerxenografts[1].AnimalModel:MicebearingHCT116humancoloncancerxenografts[1]Dosage:30,60and120mg/kgAdministration:Oralgavage,dailyfor14daysResult:Showednosignificantbodyweightchanges.Suppressedtumorgrowth.REFERENCESWangZ,etal.Design,synthesis,andantitumoractivitystudyofβ-carbolinederivativesasselectiveHDAC1/2inhibitors.BioorgChem.2025Aug;163:108763.McePdfHeight2/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalappli