BLM-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBLM-IN-1Cat.No.:HY-111756CASNo.:2056014-40-3分⼦式:C₂₈H₃₅FN₄O分⼦量:462.6作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:8.33mg/mL(18.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1617mL10.8085mL21.6169mL5mM0.4323mL2.1617mL4.3234mL10mM0.2162mL1.0808mL2.1617mL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BLM-IN-1⼀种有效的布卢姆综合征蛋⽩(BLM)抑制剂。BLM-IN-1具有⾼结合亲和⼒，KD值为1.81μM。BLM-IN-1对BLM具有良好的抑制作⽤，IC50值为0.95μM。BLM-IN-1可诱导细胞凋亡。BLM-IN-1可⽤于DNA损伤与癌症的研究。IC50&TargetIC50:0.95μM(BLM)[1].1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究BLM-IN-1(compound29)hasastrongBLMbindingwithaKDof1.81μM[1].BLM-IN-1caninhibitBLMwithanIC50of0.95μM[1].BLM-IN-1(1.0μM)inhibitstheunwindingactivityofBLMbutalsodisrupttheBLMbindingtoDNA[1].BLM-IN-1(0-1.0μM)regulatesthehomologousrecombinationbydisruptingtherecruitmentofBLMtoDSBsites[1].BLM-IN-1(1.0,2.0μM;48h)inducesDNAdamageresponseandapoptosis[1].BLM-IN-1(0.1,1.0,2.0μM;48h)inducesproliferationarrestandsyntheticinteraction[1].WesternBlotAnalysissup>[1]CellLine:HCT116cellsConcentration:0.5,1.0μMIncubationTime:24hResult:ObviouslyupregulatedthelevelofpATMandp-ATRindamageresponse.Immunofluorescence[1]CellLine:HCT116cellsConcentration:1.0μMIncubationTime:24hResult:InducedtheaccumlationofRAD51atDSBsites.CellProliferationAssay[1]CellLine:HCT116cellsConcentration:0.1,1.0,2.0μMIncubationTime:48hResult:Showedasignificantproliferationarrestinadose-dependentmannerinHCT116cells.ApoptosisAnalysis[1]CellLine:HCT116cellsConcentration:1.0,2.0μMIncubationTime:48hResult:Increasedtheratioofapoptosiscellsinaconcentration-dependentmannerandupregulatedtheexpressionlevelofcleavedcaspase-3,cleavedcaspase-7,andcleavedPARP.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].YinQK,etal.DiscoveryofIsaindigotoneDerivativesasNovelBloom'sSyndromeProtein(BLM)HelicaseInhibitorsThatDisrupttheBLM/DNAInteractionsandRegulatetheHomologousRecombinationRepair.JMedChem.2019Mar28;62(6):3147-3162.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For