LYN-1604-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELYN-1604dihydrochlorideCat.No.:HY-101923BCASNo.:2310109-38-5分⼦式:C₃₃H₄₅Cl₄N₃O₂分⼦量:657.54作⽤靶点:ULK;Autophagy;Apoptosis作⽤通路:Autophagy;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:50mg/mL(76.04mM;Needultrasonic)DMSO:50mg/mL(76.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5208mL7.6041mL15.2082mL5mM0.3042mL1.5208mL3.0416mL10mM0.1521mL0.7604mL1.5208mL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(sealedstorage,awayfrommoisture)。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.80mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(3.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LYN-1604dihydrochloride⼀种有效的UNC-51样激酶1(ULK1)激活剂，EC50值为18.94nM。LYN-1604可⽤于三性乳腺癌(TNBC)的研究[1]。IC50&TargetULK118.94nM(EC50)体外研究LYN-1604isapotentialULK1agonist(enzymaticactivity=195.7%at100nMandIC50=1.66μMagainstMDA-MB-231cells)[1].LYN-1604bindstowild-typeULK1withabindingaffinityinthenanomolerange(KD=291.4nM)[1].LYN-1604(0.5,1.0and2.0μM)inducescelldeathviatheULKcomplexinMDA-MB-231cells[1].LYN-1604(0.5-2μM,24hours)inducesremarkableup-regulationofBeclin-1anddegradationofp62,aswellastransformationofLC3-ItoLC3-IIinMDA-MB-231cells[1].LYN-1604inducesATG5-dependentautophagyviatheULKcomplex[1].LYN-1604canalsoincreasecleavageofcaspase3andinduceapoptosis[1].CellViabilityAssay[1]CellLine:MDA-MB-231cellsConcentration:0.5,1.0and2.0μMIncubationTime:Result:Inducedcelldeath.Autophagyratiowasincreasedinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0,0.5,1,and2μMIncubationTime:24hoursResult:Inducedremarkableup-regulationofBeclin-1anddegradationofp62,aswellastransformationofLC3-ItoLC3-II.体内研究LYN-1604(lowdose,25mg/kg;mediandose,50mg/kg;highdose,100mg/kg;intragastricadministrationonceadayfor14days)inhibitsthegrowthofxenograftTNBCbytargetingULK1-modulatedcelldeath[1].AnimalModel:24femalenudemice(BALB/c,6-8weeks,20-22g)[1]Dosage:Lowdose,25mg/kg;mediandose,50mg/kg;highdose,100mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intragastricadministration;onceadayfor14daysResult:SignificantlyinhibitedthegrowthofxenograftMDA-MB-231cells.Thebodyweightsofmicewerestable.Bytheendoftheexperiment,theliverandspleenweightindexesofmicewereslightlyincreasedinpartsofthegroups,whilethekidneyweightindexwasnotaffectedinalldosegroups.户使⽤本产品发表的科研⽂献•OxidMedCellLongev.15Nov2021.•BiochemJ.2019Mar12;476(5):875-887.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangL,etal.DiscoveryofasmallmoleculetargetingULK1-modulatedcelldeathoftriplenegativebreastcancerinvitroandinvivo.ChemSci.2017Apr1;8(4):2687-2701.McePdfHeightCaution:Producthasn