NiCur-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENiCurCat.No.:HY-139149分?式:C??H??N?O分?量:324.38作?靶點:HistoneAcetyltransferase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(154.14mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0828mL15.4140mL30.8280mL5mM0.6166mL3.0828mL6.1656mL10mM0.3083mL1.5414mL3.0828mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.67mg/mL(5.15mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.67mg/mL(5.15mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性NiCur?種有效的選擇性CBPhistoneacetyltransferase(HAT)抑制劑，其IC50值為0.35μΜ。NiCur阻斷CBPHAT活性，下調(diào)因毒性應激時p53的激活。NiCur可?于不響靶蛋?表達的機制研究[1]。IC50&TargetCBP0.35μM(IC50)體外研究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