MDL-800-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEMDL-800Cat.No.:HY-119376CASNo.:2275619-53-7分子式:C₂₁H₁₆BrCl₂FN₂O₆S₂分子量:626.3作用靶点:Sirtuin作用通路:CellCycle/DNADamage;Epigenetics储存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(199.58mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制备储备液1mM1.5967mL7.9834mL15.9668mL5mM0.3193mL1.5967mL3.1934mL10mM0.1597mL0.7983mL1.5967mL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方式配制澄清的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄清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是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(3.32mM);Clearsolution1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.32mM);ClearsolutionBIOLOGICALACTIVITY生物活性MDL-800是一种变构的选择性SIRT6激活剂。MDL-800增强SIRT6去乙酰化活性，EC50为10.3μM[1]。IC50&TargetSIRT610.3μM(EC50)体外研究MDL-800potentlyactivatesSIRT6at~10 µMbutshowsnoactivitytowardSIRT1,SIRT3,SIRT4,andHDAC1-11atconcentrationsupto50or100 µM.AlthoughMDL-800exhibitsweakactivitytowardSIRT2,SIRT5,andSIRT7,theEC50orIC50valuesaregreaterthan100 µM,tenfoldlessthanthatagainstSIRT6[1].MDL-800directlyactivatesSIRT6deacetylationbyincreasingthebindingaffinitiesofacetylatedsubstratesandcofactoraswellasincreasingthecatalyticefficiencyofSIRT6[1].MDL-800(1-1000μM;48hours)decreasestheproliferationofBel7405,PLC/PRF/5,andBel7402cellswithIC50sforcellgrowth(IC50-growth)of23.3μM,18.6μM,and24.0μM,respectively,andEC50sforcelldeath(EC50-death)of90.4μM,87.0μM,and106.5μM,respectively[1].MDL-800(0-50μM;24and48 hours)decreasesbothH3K9acandH3K56acataconcentrationof10µMandshowsadose-dependenteffectinBel7405,PLC/PRF/5,andBel7402cellsat24and48h[1].CellProliferationAssay[1]CellLine:Bel7405,PLC/PRF/5,andBel7402cellsConcentration:1,10,100,1000μMIncubationTime:48hoursResult:DecreasedtheproliferationofBel7405,PLC/PRF/5,andBel7402cellswithIC50sof23.3μM,18.6μM,and24.0μM,respectively.WesternBlotAnalysis[1]CellLine:Bel7405,PLC/PRF/5,andBel7402cellsConcentration:0,5,10,25,and50μMIncubationTime:24and48 hoursResult:DecreasedbothH3K9acandH3K56acataconcentrationof10µMandshowedadose-dependenteffectinallthreecelllinesat24hand48h.体内研究MDL800showseffectiveantitumorefficacyinfemaleBALB/cnudemicewithBel7405xenografttumormode.MDL800(50-150mg/kg;intraperitonealinjection;over2weeks)suppressesthegrowthofBel74052/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemExenograftsinadose-dependentmannercomparedwithvehiclealone[1].AnimalModel: Six-week-oldfemaleBALB/cnudemicewithBel7405xenografttumormode[1]Dosage: 50,100,and150mg/kgAdministration: Intraperitonealinjection;over2weeks.Result: SuppressedthegrowthofBel7405xenograftsinadose-dependentmanner.Decreasedtumorweightandsize.客户使用本产品发表的科研文献• AgingMed(Milton).2025Oct26;8(5):383-397.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HuangZ,etal.IdentificationofacellularlyactiveSIRT6allostericactivator.NatChemBiol.2018Dec;14(12):1118-1126.McePdfHeightCaution:Producthas