HDAC6-IN-65-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHDAC6-IN-65Cat.No.:HY-178110CASNo.:3028442-70-5分⼦式:C₂₀H₁₈ClN₃O₄S分⼦量:431.89作⽤靶点:HDAC;Microtubule/Tubulin;HistoneMethyltransferase作⽤通路:CellCycle/DNADamage;Epigenetics;Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性HDAC6-IN-65⼀种选择性HDAC6抑制剂(IC50=0.9nM)，同时对HDAC3也具有⼀定的抑制作⽤(IC50=39.4nM)。HDAC6-IN-65可诱导Neuro-2a细胞中α-微管蛋⽩(ac-tubulin)和⼄酰化组蛋⽩H3(ac-histoneH3，⼀种I类HDAC抑制标志物)的积累。HDAC6-IN-65可⽤于⿊⾊素瘤的研究[1]。IC50&TargetHDAC6HDAC30.9nM(IC50)39.4nM(IC50)体外研究HDAC6-IN-65(Compound14)exhibitssignificantantiproliferativeactivityagainstleukemiacellline(MV4-11,IC50=0.57μM),aswellassignificantantiproliferativeactivityagainstothertumorcells(MM.1S,IC50=2.45μM)(Neuro-2a,IC50=6.24μM)(SH-SY5Y,IC50=3.75μM),andlowtoxicitytonormalcells(HEK-293,IC50=6.09μM)(pNHF,IC50=16.24μM)(MRC9,IC50=19.08μM)[1].HDAC6-IN-65(0.05-5μM)significantlyinducestheaccumulationofα-tubulin(ac-tubulin)inNeuro-2acellsataconcentrationof50nM(amarkerofHDAC6inhibition),andacetylatedhistoneH3(ac-histoneH3,aclassIHDACinhibitionmarker)wasalsoincreasedataconcentrationof1μM[1].HDAC6-IN-65(0.5μM,6-72h),despiteitsweakerormoretransientinhibitionofclassIHDACs,mayexhibitPDeffectsthatpersistbeyonditssystemicexposureinRDEScellline[1].WesternBlotAnalysis[1]CellLine:RDEScelllineConcentration:0.5μMIncubationTime:6h,12h,24h,48h,72h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Significantlyincreasedac-tubulinlevelsinRDEScellsat6h,whichpersistuntil48h,andbegintodeclineat72h.Ac-histoneH3levelsincreasedat6and12h,butreturnedtobaselineat24h.体内研究HDAC6-IN-65(Compound14)(25mg/kg,i.p.,oncedailyfor14days,M-F)effectivelyinhibitstumorgrowthandactivatesimmuneregulationinamouseSM1melanomamodel,andshowsnosignificanttoxicitytomiceatthetestedconcentrations[1].AnimalModel:C57BL/6femalemicewereinjectedsubcutaneouslywith106invivopassagedSM1melanomacellssuspendedin100μLofPBS[1].Dosage:25mg/kgAdministration:I.p.,oncedailyfor14days,M-FResult:Themeantumorgrowthinhibitionrate(TGI)was56%.Allmiceshowednormalbodyweightandorganfunction,withnosignsoftoxicity.FlowcytometryrevealedanincreaseinCD4+andCD8+Tcells,NKcells,andM1macrophages,andadecreaseinM2macrophagesinthetumormicroenvironment.REFERENCES[1].OlaoyeOO,etal.ImprovedPharmacokineticProfilesofHDAC6InhibitorsviaCapGroupModifications.JMedChem.2025Sep11;68(17):18216-18229.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala