HDAC6-IN-4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHDAC6-IN-4Cat.No.:HY-144395CASNo.:2709103-20-6分?式:C??H??N?O?分?量:506.63作?靶點(diǎn):HDAC;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性HDAC6-IN-4(C10)?種有效的、具有?服活性的、?選擇性的HDAC6抑制劑，IC50值為23nM。HDAC6-IN-4誘導(dǎo)腫瘤細(xì)胞凋亡(apoptosis)，具有顯著的抗腫瘤作?，且?明顯毒性[1]。IC50&TargetHDAC6HDAC3HDAC2HDAC823nM(IC50)46nM(IC50)172nM(IC50)2175nM(IC50)HDAC13604nM(IC50)體外研究HDAC6-IN-4(C10)(0-50μM,72h)showsstrongantiproliferativeactivityagainstdifferentcancercellswithlowcytotoxicity[1].HDAC6-IN-4(0-6μM,24h)exhibitssignificantselectivityforHDAC6overHDAC1[1].HDAC6-IN-4inhibitsmigrationactivityinatime-dependentanddose-dependentwayinB16andCT26cells[1].HDAC6-IN-4(0-8μM,24h)inducesB16cellapoptosisinadose-dependentmanner[1].HDAC6-IN-4exhibitssignificantplasmastabilityinhumans(97%retentionafter6h),andexhibitssignificantmetabolicstabilityinhuman(half-lifeof101.91min)andmouseliver(half-lifeof67.94min)microsomes[1].CellProliferationAssay[1]CellLine:B16,HepG2,A549,andCT26cellsConcentration:0-50μM1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:72hResult:ShowedantiproliferativeactivitywithIC50valuesof1.52,2.36,5.77,and2.09μMagainstB16,HepG2,A549,andCT26cells,respectively.WesternBlotAnalysis[1]CellLine:B16andCT26cancercellsConcentration:2,4,and6μMIncubationTime:2,4,8,12,and24hResult:DramaticallyincreasedthelevelofAc-Tub(acetyl-α-tubulin)inadose-dependentandtime-dependentmanner.HadalmostnoeffectonthecontentofAc-H3(acetyl-H3).ApoptosisAnalysis[1]CellLine:B16cellsConcentration:4,6,and8μMIncubationTime:24hResult:CausedmoderatetopotentinductionofapoptosisintheB16celllineinadose-dependentmanner.UpregulatedtheexpressionofapoptoticproteincleavedPARP.體內(nèi)研究HDAC6-IN-4(C10)(0-100mg/kg;i.g.;oncedailyfor21days)showsexcellentantitumoractivityandsignificantlypromotedTcellresponseinadose-dependentmanner,withnoobvioustoxicity[1].AnimalModel:Five-week-oldC57BL/6mice(immune-relatedCT26xenograftmodel)[1].Dosage:50and100mg/kgAdministration:Oralgavage,oncedailyfor21daysResult:Resultedinasubstantialtumorgrowthandtumortissuesizeinhibitioninadose-dependentway.Showedsignificantlyhighantitumoractivity(TGI=75%)at100mg/kg.RaisedtheplasmaIFN-glevelandthenumbersofCD+andCD3+CD+(activatedcytotoxicT)cells.DecreasedCD4+CD25+CD127low/-Tregulatorycells.Showednoobvioustoxicity.REFERENCES[1].XiXu,etal.Novelbiphenyl-basedscaffoldaspotentandselectivehistonedeacetylase6(HDAC6)inhibitors:Identification,developmentandpharmacologicalevaluation.EurJMedChem.2022Apr5;233:114228.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidated