ML364-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML364Cat.No.:HY-100900CASNo.:1991986-30-1分⼦式:C₂₄H₁₈F₃N₃O₃S₂分⼦量:517.54作⽤靶点:Deubiquitinase作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥33mg/mL(63.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9322mL9.6611mL19.3222mL5mM0.3864mL1.9322mL3.8644mL10mM0.1932mL0.9661mL1.9322mL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：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:20mg/mL(38.64mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.83mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ML364⼀种泛素蛋⽩特异性肽酶(USP2)抑制剂(IC50=1.1μM)，具有抗增殖活性，可直接结合USP2(Kd=5.2μM)，诱导细胞周期蛋⽩D1降解增加并导致细胞周期停滞。ML364增加线粒体活性氧(ROS)⽔平，降低胞内ATP含量[1][2]。IC50&TargetIC50:1.1μM(USP2)[1]Kd:5.2μM(USP2)[1]体外研究ML364(5-20μM;24-48hours)inhibitsLnCAPandMCF7cellsviabilityinadose-dependentmanner[1].ML364(10μM;2-24hours)reducescyclinD1proteinlevelsinatime-,dose-,andproteasome-dependentmannerinHCT116cellsandMinocells[1].CellViabilityAssay[1]CellLine:LnCAP,MCF7cellsConcentration:5,10,15,20μMIncubationTime:24,48hoursResult:LnCAPandMCF7cellsshowedadecreaseincellviabilityinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:HCT116,MinocellsConcentration:2,4,8,16,24hoursIncubationTime:10μMResult:ReducedcyclinD1proteinlevelsinatime-,dose-,andproteasome-dependentmannerinHCT116cellsandMinocells.户使⽤本产品发表的科研⽂献•NatCommun.2022Mar31;13(1):1700.•EMBOJ.2022Jul11;e108791.•CellDeathDiffer.2020Sep;27(9):2710-2725.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JMedChem.2022Oct11.•AmJCancerRes.2021Oct15;11(10):4746-4767.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DavisMI,etal.SmallMoleculeInhibitionoftheUbiquitin-specificProteaseUSP2AcceleratescyclinD1DegradationandLeadstoCellCycleArrestinColorectalCancerandMantleCellLymphomaModels.JBiolChem.2016Nov18;291(47):24628-24640.[2].HashimotoM,etal.Inhibitionofubiquitin-specificprotease2causesaccumulationofreactiveoxygenspecies,mitochondriadysfunction,andintracellularATPdecrementinC2C12myoblasts.PhysiolRep.2019Jul;7(14):e14193.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed