ML-792-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML-792Cat.No.:HY-108702CASNo.:1644342-14-2分⼦式:C₂₁H₂₃BrN₆O₅S分⼦量:551.41作⽤靶点:E1/E2/E3Enzyme作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(181.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8135mL9.0677mL18.1353mL5mM0.3627mL1.8135mL3.6271mL10mM0.1814mL0.9068mL1.8135mL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:≥2.08mg/mL(3.77mM);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:≥2.08mg/mL(3.77mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.77mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ML-792⼀种特异性的⼩泛素样修饰物(SUMO)活化酶(SAE)抑制剂。ML-792有效选择性抑制SAE/SUMO1和SAE/SUMO2，IC50分别为3和11nM。ML-792微弱抑制NAE/NEDD8和UAE/ubiquitin，IC50分别为32μM和>100μM[1]。IC50&TargetIC50:3nM(SAE/SUMO1),11nM(SAE/SUMO2)[1]体外研究ML-792(0.0007-5μM;4hours)inhibitsSAEandSUMO-pathwayactivitiesinHCT116cells[1].ML-792(0.001-10μM;72hours)inhibitscellproliferationanddecreasescancercellviabilityinMDA-MB-468,MDA-MB-231,HCT116,Colo-205,andA375[1].CellViabilityAssay[1]CellLine:HumanbreastcancercellsMDA-MB-468andMDA-MB-231;humancoloncarcinomacellsHCT116andColo-205;humanmelanomacelllineA375Concentration:0.001,0.01,0.1,1,10μMIncubationTime:72hoursResult:Demonstratedadose-dependentviabilityeffectwithEC50valuesof0.06μMinMDA-MB-468cellsto0.45μMinA375cells.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0,0.0007,0.002,0.007,0.02,0.06,0.19,0.56,1.7,5μMIncubationTime:4hoursResult:Revealedadose-dependentdecreaseintheSAEandUBC9thioesterlevels.户使⽤本产品发表的科研⽂献•MolCell.2020Jul2;79(1):54-67.e7.•NatCommun.2022Nov11;13(1):6840.•NatCommun.2022Sep29;13(1):5726.•NatCommun.2022Sep3;13(1):5204.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellRep.2022Mar22;38(12):110534.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HeX,etal.ProbingtherolesofSUMOylationincancercellbiologybyusingaselectiveSAEinhibitor.NatChemBiol.2017Nov;13(11):1164-1171.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl