L82-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEL82Cat.No.:HY-15587CASNo.:329227-30-7分⼦式:C₁₁H₈ClN₅O₄分⼦量:309.67作⽤靶点:DNA/RNASynthesis作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(107.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2292mL16.1462mL32.2924mL5mM0.6458mL3.2292mL6.4585mL10mM0.3229mL1.6146mL3.2292mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性L82⼀种选择性的、⾮竞争性的DNA连接酶1(DNALig1)抑制剂(hLig1IC50=12μM)。L82对乳腺癌细胞显⽰出抗增殖活性。体外研究L82(0-50μM;6d)showsanti-proliferativeactivitytobreastcancercells[2].L82(50μM;0-48h)showscytostaticactivityduetoactivationoftheG1/ScheckpointinMCF7cells[2].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellProliferationAssay[2]CellLine:MCF10A,MCF7,HCT116,andHeLacellsConcentration:0-50μMIncubationTime:6daysResult:ReducedtheproliferationofanormalbreastepithelialcelllineMCF10AandthebreastcancercelllinesMCF7,HeLaandHCT116,inaconcentration-dependentmanner.CellCycleAnalysis[2]CellLine:MCF7cellsConcentration:50μMIncubationTime:0-48hoursResult:ShowedatransientaccumulationofcellsatG2/Mafter12h,thenshowedanaccumulationatG0/G1thatpeakedafter24h.DecreasedintheSphasecellinaccompanywiththeincreaseintheG0/G1phase.REFERENCES[1].HowesTRL,etal.Structure-activityrelationshipsamongDNAligaseinhibitors:CharacterizationofaselectiveuncompetitiveDNAligaseIinhibitor.DNARepair(Amst).2017Dec;60:29-39.[2].ChenX,etal.RationaldesignofhumanDNAligaseinhibitorsthattargetcellularDNAreplicationandrepair.CancerRes.2008May1;68(9):3169-77.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8