CPTH2-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECPTH2hydrochlorideCat.No.:HY-W013274ACASNo.:2108899-91-6分⼦式:C₁₄H₁₅Cl₂N₃S分⼦量:328.26作⽤靶点:HistoneAcetyltransferase;Apoptosis作⽤通路:Epigenetics;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CPTH2hydrochloride有效的组蛋⽩⼄酰转移酶(HAT)抑制剂。CPTH2hydrochloride选择性地抑制Gcn5对组蛋⽩H3的⼄酰化。CPTH2hydrochloride通过抑制⼄酰转移酶p300(KAT3B)诱导凋亡(apoptosis)并降低透明细胞肾癌(ccRCC)细胞系的侵袭性。IC50&TargetGCN5p300体外研究CPTH2(100μM;12,24,48hours)hydrochloridecausesadecreaseincellproliferationafterasearlyas12hwithafurthersignificantreductionafter48hstimulation[1].CPTH2(100μM;12or48hours)hydrochloridecausesacomparabledropoftheactivityinbothcelllines[1].CPTH2(100μM;48hours)hydrochlorideproducesadrasticincreaseinapoptotic/deadcellpopulationafter48h[1].CPTH2(100μM;12,24,48hours)hydrochlorideshowsareducedacetylationofbothglobalAcH3histoneandH3AcK18[1].CPTH2(100μM;24,48hours)hydrochlorideiscapabletocounteractinvasionandmigrationofccRCC-786-Ocellsinculture[1].CPTH2(0.2,0.5,1mM)hydrochlorideinhibitsthegrowthofaGCN5deletedstrainandasinglecatalyticmutantE173H[2].CPTH2(0.6,0.8mM;for24hours)hydrochlorideinhibitshistoneH3acetylationinyeastcellcultures[2].CPTH2hydrochlorideinhibitstheGcn5pdependentfunctionalnetwork[2].CellProliferationAssay[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:Papillarythyroid(K1)andclearcellRenalCellCarcinoma(ccRCC-786-O)celllinesConcentration:100μMIncubationTime:12,24,48hoursResult:Causedadecreaseincellproliferationafterasearlyas12hwithafurthersignificantreductionafter48hstimulation.CellViabilityAssay[1]CellLine:K1andccRCC-786-OcelllinesConcentration:100μMIncubationTime:24hours(K1cell)and48hours(ccRCC-786-Ocell)Result:Causedacomparabledropoftheactivityinbothcelllines.ApoptosisAnalysis[1]CellLine:ccRCC-786-OcellsConcentration:100μMIncubationTime:48hoursResult:Producedadrasticincreaseinapoptotic/deadcellpopulationafter48h.WesternBlotAnalysis[1]CellLine:ccRCC-786-OcellsConcentration:100μMIncubationTime:12,24,48hoursResult:ShowedareducedacetylationofbothglobalAcH3histoneandH3AcK18.REFERENCES[1].CoccoE,etal.KAT3B-p300andH3AcK18/H3AcK14levelsareprognosticmarkersforkidneyccRCCtumoraggressivenessandtargetofKATinhibitorCPTH2.ClinEpigenetics.2018Apr4;10:44.[2].ChimentiF,etal.AnovelhistoneacetyltransferaseinhibitormodulatingGcn5network:cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone.JMedChem.2009Jan22;52(2):530-6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical