LV-320-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELV-320Cat.No.:HY-112711CASNo.:2449093-46-1分⼦式:C₂₉H₂₆ClNO₂S₂分⼦量:520.11作⽤靶点:Autophagy;Cathepsin作⽤通路:Autophagy;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:135mg/mL(259.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9227mL9.6134mL19.2267mL5mM0.3845mL1.9227mL3.8453mL10mM0.1923mL0.9613mL1.9227mL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。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:≥2.25mg/mL(4.33mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.25mg/mL(4.33mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LV-320⼀种有效且⾮竞争性的ATG4B抑制剂，其IC50值为24.5μM，Kd值为16μM。LV-320抑制ATG4B的酶促活性，阻断细胞⾃噬，并且在体内稳定，⽆毒且有活性。IC50&TargetIC50:24.5ꢀµM(ATG4B);Kd:16μM(ATG4B)[1]体外研究LV-320(0-120ꢀµM;SKBR3,MCF7,JIMT1,andMDA-MB-231cells)treatmentresultsinadose-dependentincreaseinendogenousLC3B-IIandproteinp62levelsinallfourcelllines[1].LV-320(120ꢀµM;48hours;MDA-MB-231cells)treatmentresultsinanincreaseinLC3B-II,indicatingthatLV-320blocksautophagicflux[1].WesternBlotAnalysis[1]CellLine:SKBR3,MCF7,JIMT1,andMDA-MB-231cellsConcentration:0ꢀµM,25ꢀµM,50ꢀµM,75ꢀµM,100ꢀµM,or120ꢀµMIncubationTime:Result:Resultedinadose-dependentincreaseinendogenousLC3B-IIandproteinp62levelsinallfourcelllines.CellAutophagyAssay[1]CellLine:MDA-MB-231cellsConcentration:120ꢀµMIncubationTime:48hoursResult:Blockedautophagicflux.体内研究LV-320(100-200ꢀmg/kg;oralgavage;threetimesovertwodays;GFP-LC3mice)treatmentresultsinaterminalbloodlevelof169µMandaliverlevelof104µM.TheexpressionofGFP-LC3punctaissignificantlygreateraccumulationinLV-320treatedanimalscomparedtocontrols.LC3B-IIproteinisalsoincreasedinLV-320-treatedanimals.Thetreatmentdonotcausesignificanttoxicityinmiceateitherdose[1].AnimalModel:GFP-LC3mice(females,9-14weeks)[1]Dosage:100ꢀmg/kgor200ꢀmg/kgAdministration:Oralgavage;threetimesovertwodays(Pharmacokineticstudy)2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Terminalbloodlevelswere169ꢀµMandliverlevelswere104ꢀµM.LC3B-IIproteinlevelwasalsoincreased.REFERENCES[1].BoscD,etal.Anewquinoline-basedchemicalprobeinhibitstheautophagy-relatedcysteineproteaseATG4B.SciRep.2018Aug3;8(1):11653.doi:10.1038/s41598-018-29900-x.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed