Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEMDL-800Cat.No.:HY-119376CASNo.:2275619-53-7分子式:C??H??BrCl?FN?O?S?分子量:626.3作用靶點(diǎn):Sirtuin作用通路:CellCycle/DNADamage;Epigenetics儲(chǔ)存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(199.58mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.5967mL7.9834mL15.9668mL5mM0.3193mL1.5967mL3.1934mL10mM0.1597mL0.7983mL1.5967mL請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存方式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊?qǐng)先按照InVitro方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.32mM);Clearsolution1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.32mM);ClearsolutionBIOLOGICALACTIVITY生物活性MDL-800是一種變構(gòu)的選擇性SIRT6激活劑。MDL-800增強(qiáng)SIRT6去乙?；钚?，EC50為10.3μM[1]。IC50&TargetSIRT610.3μM(EC50)體外研究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.體內(nèi)研究MDL800showseffectiveantitumorefficacyinfemaleBALB/cnudemicewithBel7405xenografttumormode.MDL800(50-150mg/kg;intraperitonealinjection;over2weeks)suppressesthegrowthofBel74052/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemExenograftsinadose-dependentmannercomparedwithvehiclealone[1].AnimalModel: Six-week-oldfemaleBALB/cnudemicewithBel7405xenografttumormode[1]Dosage: 50,100,and150mg/kgAdministration: Intraperitonealinjection;over2weeks.Result: SuppressedthegrowthofBel7405xenograftsinadose-dependentmanner.Decreasedtumorweightandsize.客戶(hù)使用本產(chǎn)品發(fā)表的科研文獻(xiàn)? AgingMed(Milton).2025Oct26;8(5):383-397.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HuangZ,etal.IdentificationofacellularlyactiveSIRT6allostericactivator.NatChemBiol.2018Dec;14(12):1118-1126.McePdfHeightCaution:Producthas