HDAC-IN-94-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEHDAC-IN-94Cat.No.:HY-179019分子式:C₁₈H₁₈N₂O₅分子量:342.35作用靶点:HDAC;Microtubule/Tubulin;Apoptosis;Caspase作用通路:CellCycle/DNADamage;Epigenetics;Cytoskeleton;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性HDAC-IN-94是一种强效、选择性的HDAC6抑制剂(IC50=4.5nM)。HDAC-IN-94对HDAC6的选择性是对HDAC8的1000倍以上，并且对其他亚型(HDAC1-3,10)的活性极弱。HDAC-IN-94诱导α-微管蛋白(α-tubulin)的超乙酰化、细胞凋亡(apoptosis)和G2/M期细胞周期阻滞，有强大对抗肿瘤功效和较低的细胞毒性。HDAC-IN-94可用于神经母细胞瘤和胶质母细胞瘤的相关研究[1]。IC50&TargethHDAC6hHDAC8hHDAC1hHDAC104.5nM(IC50)3273nM(IC50)403nM(IC50)202nM(IC50)hHDAC2hHDAC3hHDAC5hHDAC11537nM(IC50)1278nM(IC50)4455nM(IC50)>10000nM(IC50)体外研究HDAC-IN-94(compound5o)fitswithinthecatalyticsiteofhHDAC6withthehydroxamicacidgroup,modelledinneutralform,abletochelatethezincatom,anditspolarbenzamidehydrogenformingahydrogenbondwithSer568[1].HDAC-IN-94(1-10μM,24h)promotesacetylationofα-tubulininadose-dependentmannerinSH-SY5Ycells[1].HDAC-IN-94(10nM-30μM,24-72h)showsnocytotoxicityinHEK-293cellsatconcentrationsupto30μM[1].HDAC-IN-94(24-72h)showsantiproliferationactivityagainstU87-MG,T98G,U251-MGandSH-SY5Ycells,withIC50sof51.31,42.60,2.37,and3.32μM,respectively[1].HDAC-IN-94(3μM,24h)promotesG2/Mcellcyclearrest,triggersprogrammedcelldeath,andinducesaminorautophagystimulationinSH-SY5Ycells[1].HDAC-IN-94(3-30μM,24-72h)demonstratesacleartime-andconcentration-dependentpro-apoptoticactivityinSH-SY5Ycells[1].1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEWesternBlotAnalysis[1]CellLine:SH-SY5YcellsConcentration:1and10μMIncubationTime:24hResult:Promotedacetylationofα-tubulininadose-dependentmanner.CellCycleAnalysis[1]CellLine:SH-SY5YcellsConcentration:3μMIncubationTime:24hResult:LedtoanaccumulationofhypodiploidSH-SY5YcellsinthesubG0/G1phase.ShowedadecreaseintheG0/G1populationandaslightincreaseincellswithintheS-phase.ApoptosisAnalysis[1]CellLine:SH-SY5YcellsConcentration:3,10,and30μMIncubationTime:24,48and72hResult:Inducedaconcentration-dependentincreaseinearlyapoptosisat24h.Inducedasignificantincreaseoflateapoptosisstartingat10μM(24h).Showedsignificanteffectsonbothearlyandlateapoptosisat10μMandapronouncedapoptoticresponseat30μM(46%forearlyand27%forlateapoptosis),at48hoftreatment.Significantlyincreasedearlyandlateapoptosisatallconcentrationsat72h.Inducedaconcentration-dependentincreaseincaspase-3/7activation,startingfrom10μMat24h.Elicited24%caspase-positivecellsat30μMat24h.Showedasignificantincreaseincaspaseactivationat10μMand30μMat48h.Continuedtoactivatecaspase-3/7inaconcentration-dependentmannerafter72h,with43%positivityat30μM.REFERENCESCursaroI,etal.NewVanillyl-cappedHDACinhibitorsexhibitanti-tumorefficacyinneuroblastomaandglioblastomacells.BioorgChem.2025Oct14;166:109085.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyv