ML364-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML364Cat.No.:HY-100900CASNo.:1991986-30-1分?式:C??H??F?N?O?S?分?量:517.54作?靶點:Deubiquitinase作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥33mg/mL(63.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9322mL9.6611mL19.3222mL5mM0.3864mL1.9322mL3.8644mL10mM0.1932mL0.9661mL1.9322mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:20mg/mL(38.64mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.83mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.83mM);ClearsolutionBIOLOGICALACTIVITY?物活性ML364?種泛素蛋?特異性肽酶(USP2)抑制劑(IC50=1.1μM)，具有抗增殖活性，可直接結(jié)合USP2(Kd=5.2μM)，誘導(dǎo)細(xì)胞周期蛋?D1降解增加并導(dǎo)致細(xì)胞周期停滯。ML364增加線粒體活性氧(ROS)?平，降低胞內(nèi)ATP含量[1][2]。IC50&TargetIC50:1.1μM(USP2)[1]Kd:5.2μM(USP2)[1]體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻?NatCommun.2022Mar31;13(1):1700.?EMBOJ.2022Jul11;e108791.?CellDeathDiffer.2020Sep;27(9):2710-2725.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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