HDAC6-IN-69-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHDAC6-IN-69Cat.No.:HY-180214分⼦式:C₁₇H₁₇BrN₂O₄S分⼦量:425.3作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性HDAC6-IN-69⼀种可透过⾎脑屏障、⾼选择性的HDAC6抑制剂，其IC50为4.0nM，对其他HDAC亚型的选择性超过176倍。HDAC6-IN-69能在神经元细胞中剂量依赖性地上调⼄酰化α-微管蛋⽩⽔平，从⽽发挥神经保护作⽤，可⽤于缺⾎性中风研究[1]。IC50&TargetHDAC1HDAC3HDAC4HDAC61135nM(IC50)9.0nM(IC50)1248nM(IC50)4.0nM(IC50)HDAC8HDAC11702.5nM(IC50)1243.0nM(IC50)体外研究HDAC6-IN-69(compound8k)demonstratesafavorablepharmacokineticprofilewithmoderateclearanceandmetabolicstabilityinbothhumanandratlivermicrosomes(T1/2inHLM=154.00min,T1/2inRLM=29.49min),alongwithalowriskofcardiotoxicity.[1].HDAC6-IN-69(1.0-10μM,24h)selectivelyinhibitHDAC6ratherthanHDAC1inhumanneuroblastomacells(SH-SY5Ycells)[1].HDAC6-IN-69(0.1-10μM,0.5h)haspotentialneuroprotectiveactivityinL-glutamate(HY-N0455B)induced-SH-SY5Ycells[1].CellViabilityAssay[1]CellLine:HumanneuroblastomacellsConcentration:0.1μM,1μM,10μMIncubationTime:24h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:EfficientlytransportedtoSH-SY5Ycellsandupregulatedtheexpressionofacetylatedα-tubulininadose-dependentmanner,whiletheexpressionofacetylatedhistoneH3wasonlymoderatelyaffectedCellCytotoxicityAssay[1]CellLine:L-glutamateinduced-SH-SY5YcellsConcentration:0.1μM,1μM,10μMIncubationTime:0.5hResult:IncreasedthesurvivalrateofdamagedcellsatlowandmediumdosesExhibitmorestableneuroprotectiveactivityandawidetherapeuticrangeShowedadownwardtrendathighconcentrationsShowedahighcellsurvivalrateathighconcentrations体内研究HDAC6-IN-69(compound8k)(6or12.5mg/kg,i.v.,once)showsagreatpotentialforalleviatingstroke-inducedbraininfarctioninMCAOratmodel[1].AnimalModel:Ischemiainduced(anylonthreadwasgentlyinsertedfromthecommoncarotidarteryintothemiddlecerebralarteryfor1.5hours)-maleSprague-Dawley(SD)rats(240g)[1].Dosage:6or12.5mg/kgAdministration:i.v.,onceResult:Reducedthecerebralinfarctionarea(from32.87%to13.13%).REFERENCES[1].BoHan,etal.Metabolism-BasedDrugDiscovery:NovelBenzothiazepine-ContainingHDAC6InhibitorasaPotentialNeuroprotectiveAgent.ACSMedicinalChemistryLetters.5,2026McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For