C646-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEC646Cat.No.:HY-13823CASNo.:328968-36-1分⼦式:C₂₄H₁₉N₃O₆分⼦量:445.42作⽤靶点:HistoneAcetyltransferase;Autophagy;EpigeneticReaderDomain;Apoptosis作⽤通路:Epigenetics;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months

-20°C1month溶解性数据体外实验DMSO:16.67mg/mL(37.43mM;Needultrasonic)扫描⼆维码，运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2451mL11.2254mL22.4507mL5mM0.4490mL2.2451mL4.4901mL10mM0.2245mL1.1225mL2.2451mL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。BIOLOGICALACTIVITY⽣物活性C646⼀种竞争性的选择性histoneacetyltransferasep300抑制剂，Ki值为400nM，对其他的⼄酰转移酶作⽤较⼩[1]。IC50&TargetKi:400nM(histoneacetyltransferasep300)体外研究C646isalinearcompetitiveinhibitorofp300versusacetyl-CoAwithaKiof400nM.C646showsanoncompetitivepatternofp300inhibitionversusH4-15peptidesubstrate.C646treatmentreduceshistone1/3www.MedChemEwww.MedChemEH3andH4acetylationlevelsandabrogatesTSA-inducedacetylationincells.C646hasamorepotenteffectoncellgrowththanLys-CoA-Tatdoes[1].C646enhancesmitoticcatastropheafterIRandsuppressesphosphorylationofCHK1afterIRinA549cells[2].C646attenuatestheincreasedacetylationofGATA1andtheincreasedtranscriptionalactivityofGATA1inducedbyEDAG[3].体内研究SuppressionofP300byc646(intraperitoneallyinjected,30nmol/g/dfor2weeks)dramaticallyreducesthelevelofbloodglucoseindb/dbmice[4].AnimalModel:Fourteen-week-oldmaledb/dbmiceandnormalm/mmice[4]Dosage:30nmol/gAdministration:Intraperitoneallyinjected;daily;2weeksResult:Thedb/dbmiceshowedgreaterbodymassesandhigherlevelsoffastingbloodglucosethanthem/mmice.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2019Mar18;47(5):2455-2471.•CellDeathDiffer.2018Nov;25(11):1980-1995.•Theranostics.2021Jan1;11(3):1473-1492.•Oncogene.2021Mar12.•MolTherNucleicAcids.2021Jan1;23:667-681.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BowersEM,etal.Virtualligandscreeningofthep300/CBPhistoneacetyltransferase:identificationofaselectivesmallmoleculeinhibitor.ChemBiol.2010May28;17(5):471-82.[2].OikeT,etal.C646,aselectivesmallmoleculeinhibitorofhistoneacetyltransferasep300,radiosensitizeslungcancercellsbyenhancingmitoticcatastrophe.RadiotherOncol.2014May;111(2):222-7.[3].ZhengWW,etal.EDAGpositivelyregulateserythroiddifferentiationandmodifiesGATA1acetylationthroughrecruitingp300.StemCells.2014Aug;32(8):2278-89.[4].ZhenFan,etal.Type2diabetes-inducedoveractivationofP300contributestoskeletalmuscleatrophybyinhibitingautophagicflux.LifeSci.2020Aug10;258:118243.McePdfHeight2/3www.MedChemEwww.MedChemE关注MCE中国公众号，

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