NiCur-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENiCurCat.No.:HY-139149分⼦式:C₂₂H₁₆N₂O分⼦量:324.38作⽤靶点:HistoneAcetyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(154.14mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0828mL15.4140mL30.8280mL5mM0.6166mL3.0828mL6.1656mL10mM0.3083mL1.5414mL3.0828mL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%salineSolubility:≥1.67mg/mL(5.15mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.67mg/mL(5.15mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性NiCur⼀种有效的选择性CBPhistoneacetyltransferase(HAT)抑制剂，其IC50值为0.35μΜ。NiCur阻断CBPHAT活性，下调因毒性应激时p53的激活。NiCur可⽤于不响靶蛋⽩表达的机制研究[1]。IC50&TargetCBP0.35μM(IC50)体外研究NiCur(0.5~1μM;U2OScells)reducestheDox-inducedp53K382ac,p53S15p,andp53levelsinadose-dependentmanner[1].NiCur(1.5μM)reducesthelevelofH3K27ac.NiCur(1.5μM;U2OScells)restorescellularproliferation.NiCur(Intestinalepithelialcells)down-regulatesDox-mediatedp53activationwithoutaffectingthelevelsofH2A.XS139p.NiCurcanmodulatethegeneregulatoryswitchforreprogrammingchromatinlandscape.NiCurblocksCBPHATactivity[1].WesternBlotAnalysis[1]CellLine:U2OScellsConcentration:0.5~1μMIncubationTime:Result:ReducedtheDox-inducedp53K382ac,p53S15p,andp53levelsinadose-dependentmanner.REFERENCES[1].VincekAS,etal.InhibitorofCBPHistoneAcetyltransferaseDownregulatesp53ActivationandFacilitatesMethylationatLysine27onHistoneH3.Molecules.2018;23(8):1930.Published2018Aug2.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl