CPTH2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemECPTH2Cat.No.:HY-W013274CASNo.:357649-93-5分⼦式:C₁₄H₁₄ClN₃S分⼦量:291.8作⽤靶点:HistoneAcetyltransferase;Apoptosis作⽤通路:Epigenetics;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(85.68mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)Ethanol:1mg/mL(3.43mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4270mL17.1350mL34.2701mL5mM0.6854mL3.4270mL6.8540mL10mM0.3427mL1.7135mL3.4270mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.57mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性CPTH2有效的组蛋⽩⼄酰转移酶(HAT)抑制剂。CPTH2选择性地抑制Gcn5对组蛋⽩H3的⼄酰化。CPTH2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)causesadecreaseincellproliferationafterasearlyas12hwithafurthersignificantreductionafter48hstimulation[1].CPTH2(100μM;12or48hours)causesacomparabledropoftheactivityinbothcelllines[1].CPTH2(100μM;48hours)producesadrasticincreaseinapoptotic/deadcellpopulationafter48h[1].CPTH2(100μM;12,24,48hours)showsareducedacetylationofbothglobalAcH3histoneandH3AcK18[1].CPTH2(100μM;24,48hours)iscapabletocounteractinvasionandmigrationofccRCC-786-Ocellsinculture[1].CPTH2(0.2,0.5,1mM)inhibitsthegrowthofaGCN5deletedstrainandasinglecatalyticmutantE173H[2].CPTH2(0.6,0.8mM;for24hours)inhibitshistoneH3acetylationinyeastcellcultures[2].CPTH2inhibitstheGcn5pdependentfunctionalnetwork[2].CellProliferationAssay[1]CellLine: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:48hours2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEResult: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:Producthasnotbeenfu