C646-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.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)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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:1.67mg/mL(3.75mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.67mg/mL(3.75mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY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.C646treatmentreduceshistoneH3andH4acetylationlevelsandabrogatesTSA-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•NatMicrobiol.2021Jul;6(7):932-945.•NucleicAcidsRes.2019Mar18;47(5):2455-2471.•JExpClinCancerRes.2021May10;40(1):162.•CellDeathDiffer.2018Nov;25(11):1980-1995.•Theranostics.2021Jan1;11(3):1473-1492.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BowersEM,etal.Virtualligandscreeningofthep300/CBPhistoneacetyltransferase:identificationofaselectivesmallmolecule2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEinhibitor.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.McePdfHeightCaution:Producthasnotbe