Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBLM-IN-1Cat.No.:HY-111756CASNo.:2056014-40-3分?式:C??H??FN?O分?量:462.6作?靶點(diǎn):Apoptosis作?通路:Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:8.33mg/mL(18.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1617mL10.8085mL21.6169mL5mM0.4323mL2.1617mL4.3234mL10mM0.2162mL1.0808mL2.1617mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性BLM-IN-1?種有效的布盧姆綜合征蛋?(BLM)抑制劑。BLM-IN-1具有?結(jié)合親和?，KD值為1.81μM。BLM-IN-1對(duì)BLM具有良好的抑制作?，IC50值為0.95μM。BLM-IN-1可誘導(dǎo)細(xì)胞凋亡。BLM-IN-1可?于DNA損傷與癌癥的研究。IC50&TargetIC50:0.95μM(BLM)[1].1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究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?邊的抑制劑?師www.MedChemEREFERENCES[1].YinQK,etal.DiscoveryofIsaindigotoneDerivativesasNovelBloom'sSyndromeProtein(BLM)HelicaseInhibitorsThatDisrupttheBLM/DNAInteractionsandRegulatetheHomologousRecombinationRepair.JMedChem.2019Mar28;62(6):3147-3162.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For