Lys05-Lys01-trihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELys05Cat.No.:HY-12855ACASNo.:1391426-24-6Synonyms:Lys01trihydrochloride分⼦式:C₂₃H₂₆Cl₅N₅分⼦量:549.75作⽤靶点:Autophagy作⽤通路:Autophagy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DMSO:25mg/mL(45.48mM;ultrasonicandadjustpHto2withHCl)H2O:6.4mg/mL(11.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8190mL9.0950mL18.1901mL5mM0.3638mL1.8190mL3.6380mL10mM0.1819mL0.9095mL1.8190mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥4.17mg/mL(7.59mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.55mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥7.5mg/mL(13.64mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Lys05(Lys01trihydrochloride)新颖的溶酶体⾃噬(lysosomalautophagy)抑制剂。在MTT试验中，对1205Lu,c8161,LN229和HT-29细胞系的IC50值分别为3.6,3.8,6和7.9μM。IC50&TargetIC50:3.6μM(1205Lu),3.8μM(c8161),6μM(LN229),7.9μM(HT-29)[1]体外研究Lys01,isa10-foldmorepotentautophagyinhibitorthanHCQ.ComparedwithHCQ,Lys05,awater-solublesaltofLys01,morepotentlyaccumulateswithinanddeacidifiesthelysosome.Lys01andLys05produceequivalentdose-dependentincreasesintheLC3II/LC3Iratio,accumulationoftheautophagycargoproteinp62,andidenticalIC50valuesintheMTTassay[1].体内研究Withthishigh-dose,short-termtreatment,nomicedie,butafter2dofdosing,micetreatedwithLys0576mg/kgi.p.areobservedtohavearchedbacksandlethargy.Morphologically,EMshowthatcellswithintactnuclearandcytoplasmicmembranescontainlargeAVsinLys05-treatedtumors.TumorgrowthissignificantlyimpairedinLys05-treatedtumorscomparedwithcontrols.Lys05treatmentresultsina53%reductionintheaveragedailytumorgrowthratecomparedwithvehicle-treatedcontrols.Asignificantthree-andsix-foldaccumulationofAVisobservedattheendof14doftreatmentinHCQ-andLys05-treatedtumors,respectively,comparedwithcontrol-treatedtumors[1].PROTOCOLCellAssay[1]1205Lu,c8161,LN229andHT-29cellsaretreatedwithLys05(0,0.01,0.1,1,and10μM)orLys01(0,0.01,0.1,1,and10μM)infivereplicatesfor72h.TheAcidPhsophataseAssaykitisusedfortheMTTassay[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:ToinvestigatethesafetyofLys05anditsinvivoeffectsonautophagy,c8161xenograftsmatchedforAdministration[1]tumorsizearetreatedwithi.p.dailyPBS,orequimolardosesofHCQorLys05[HCQ60mg/kg(138nM/g),Lys0576mg/kg(138nM/g)]for48h[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•EnvironToxicol.2021Dec7.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].McAfeeQ,etal.AutophagyinhibitorLys05hassingle-agentantitumoractivityandreproducesthephenotypeofageneticautophagydeficiency.ProcNatlAcadSciUSA.2012May22;109(21):8253-8.McePdfHeightCaution:Prod