S130-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemES130Cat.No.:HY-112818CASNo.:1160852-22-1分⼦式:C₂₄H₂₅N₃O₂分⼦量:387.47作⽤靶点:Cathepsin;Autophagy;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(322.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5808mL12.9042mL25.8084mL5mM0.5162mL2.5808mL5.1617mL10mM0.2581mL1.2904mL2.5808mL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(5.81mM);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%(20%SBE-β-CDinsaline)Solubility:≥2.25mg/mL(5.81mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性S130⼀种⾼亲和⼒、选择性的半胱氨酸蛋⽩酶ATG4B的抑制剂,IC50值为3.24µM。S130可以抑制⾃噬通量[1]。IC50&TargetIC50:3.24µM(ATG4B)[1]体外研究S130suppressesautophagyandactivatesapoptosisbyinhibitingATG4B,leadstoenhancedcytotoxicity[1].S130(10μM;6hours)suppressesautophagyattheearlyLC3primingsteporlateautolysosomedegradationstage[1].S130accumulatesautolysosomeswithmorelipidatedLC3[1].S130(0-25μM;48hours)inducescelldeaththroughinhibitingtheactivityofATG4Batadosehigherthan6.3µM.Andsuchcytotoxicitymightnotcausecelldeaththroughnecroptosis[1].NutrientdeprivationenhancesS130-inducedcytotoxicity[1].S130(0-10μM;24hours)suppressesapproximately79%ofthecleavageoffull-lengthLC3-GSTatthe10µM,whilenosubstrateswereprocessedinATG4BKOcells.S130displaysobviousinhibitoryeffectsonATG4B[1].CellCytotoxicityAssay[1]CellLine:HeLacells,HCT116cells,HL60cellsConcentration:0μM,3.1μM,6.3μM,12.5μM,25μMIncubationTime:48hoursResult:HadsignificantcytotoxiceffectsonHeLacells(IC50=16.1µM),HCT116cells(IC50=9.0µM)andHL60cells(IC50=4.7µM)atadosehigherthan6.3µM.Andsuchcytotoxicitymightnotcausecelldeaththroughnecroptosis.CellAutophagyAssay[1]CellLine:HeLacellsandMEFcellsConcentration:10μMIncubationTime:6hoursResult:SuppressedautophagyattheearlyLC3primingsteporlateautolysosomedegradationstage.WesternBlotAnalysis[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HeLacellsConcentration:0μM,5μM,10μMIncubationTime:24hoursResult:Suppressedapproximately79%ofthecleavageoffull-lengthLC3-GSTat10µM,whilenosubstrateswereprocessedinATG4BKOcells.体内研究S130(20mg/kg;i.p.;daily;3weeks)suppressestumorgrowth,andshowsanefficientinvivoantitumoreffectwithasoundsafetyonvitalorgans[1].AnimalModel:BALB/cnudefemalemice(4weeks),withHCT116cellsxenograft[1]Dosage:20mg/kgAdministration:Intraperitonealinjection;daily;3weeksResult:Wasabletosuppresstumorgrowthandwithasoundsafetyonvitalorgans.REFERENCES[1].FuY,etal.DiscoveryofasmallmoleculetargetingautophagyviaATG4Binhibitionandcelldeathofcolorectalcancercellsinvitroandinvivo.Autophagy.2018Sep20:1-17.McePdfHeightCaution:Producthas