LV-320-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELV-320Cat.No.:HY-112711CASNo.:2449093-46-1分?式:C??H??ClNO?S?分?量:520.11作?靶點(diǎn):Autophagy;Cathepsin作?通路:Autophagy;MetabolicEnzyme/Protease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:135mg/mL(259.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9227mL9.6134mL19.2267mL5mM0.3845mL1.9227mL3.8453mL10mM0.1923mL0.9613mL1.9227mL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?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.25mg/mL(4.33mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.25mg/mL(4.33mM);ClearsolutionBIOLOGICALACTIVITY?物活性LV-320?種有效且?競(jìng)爭(zhēng)性的ATG4B抑制劑，其IC50值為24.5μM，Kd值為16μM。LV-320抑制ATG4B的酶促活性，阻斷細(xì)胞?噬，并且在體內(nèi)穩(wěn)定，?毒且有活性。IC50&TargetIC50:24.5?μM(ATG4B);Kd:16μM(ATG4B)[1]體外研究LV-320(0-120?μM;SKBR3,MCF7,JIMT1,andMDA-MB-231cells)treatmentresultsinadose-dependentincreaseinendogenousLC3B-IIandproteinp62levelsinallfourcelllines[1].LV-320(120?μM;48hours;MDA-MB-231cells)treatmentresultsinanincreaseinLC3B-II,indicatingthatLV-320blocksautophagicflux[1].WesternBlotAnalysis[1]CellLine:SKBR3,MCF7,JIMT1,andMDA-MB-231cellsConcentration:0?μM,25?μM,50?μM,75?μM,100?μM,or120?μMIncubationTime:Result:Resultedinadose-dependentincreaseinendogenousLC3B-IIandproteinp62levelsinallfourcelllines.CellAutophagyAssay[1]CellLine:MDA-MB-231cellsConcentration:120?μMIncubationTime:48hoursResult:Blockedautophagicflux.體內(nèi)研究LV-320(100-200?mg/kg;oralgavage;threetimesovertwodays;GFP-LC3mice)treatmentresultsinaterminalbloodlevelof169μMandaliverlevelof104μM.TheexpressionofGFP-LC3punctaissignificantlygreateraccumulationinLV-320treatedanimalscomparedtocontrols.LC3B-IIproteinisalsoincreasedinLV-320-treatedanimals.Thetreatmentdonotcausesignificanttoxicityinmiceateitherdose[1].AnimalModel:GFP-LC3mice(females,9-14weeks)[1]Dosage:100?mg/kgor200?mg/kgAdministration:Oralgavage;threetimesovertwodays(Pharmacokineticstudy)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Terminalbloodlevelswere169?μMandliverlevelswere104?μM.LC3B-IIproteinlevelwasalsoincreased.REFERENCES[1].BoscD,etal.Anewquinoline-basedchemicalprobeinhibitstheautophagy-relatedcysteineproteaseATG4B.SciRep.2018Aug3;8(1):11653.doi:10.1038/s41598-018-29900-x.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed