Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENMDI14Cat.No.:HY-111374CASNo.:307519-88-6分?式:C??H??N?O?S分?量:415.51作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥25mg/mL(60.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4067mL12.0334mL24.0668mL5mM0.4813mL2.4067mL4.8134mL10mM0.2407mL1.2033mL2.4067mL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(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:0.83mg/mL(2.00mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.83mg/mL(2.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性NMDI14?種?義介導(dǎo)的RNA衰變(NMD)抑制劑。NMDI14?擾SMG7-UPF1相互作?，抑制?義介導(dǎo)的RNA衰變。IC50&TargetNMD[1]體外研究NMDI14isanonsensemediatedRNAdecay(NMD)inhibitor.TreatingcellswithNMDI14for6hoursleadstoanincreaseofPTC39βglobinto12%,arelativefour-foldincreasethat,ifresultinginbiologicallyactivehemoglobin,wouldbesufficienttoamelioratetheclinicalsymptomsofthalassemia.ThreedaysoftreatmentwithNMDI14resultsinnodecreaseincellcounts,demonstratingthatthepharmacologicalinhibitionofNMDcanbeachievedwithoutsubtlechangesinproliferation.941genesareincreased>1.5foldwithNMDI14.ThetreatmentofN417cellswithNMDI14for6hoursleadstoasteadystateexpressionofp53similartothatseeninU2OScells.NMDI14significantlyincreasesthestabilityofPTCmutatedp53mRNAinN417cells,withoutalteringthestabilityofwild-typep53inNMDItreatedU2OScells[1].PROTOCOLCellAssay[1]Toassessviabilitycellsareculturedin6welldishesandincubatedwithDMSO,G418,NMDIaloneorG418withNMDItogetherfortheindicatedhours.Afterincubations,cellsandmediaarecollectedandcellsviabilityismeasured.ToassesscellproliferationU2OS,HelaandBJ-htertcellsareculturedin6wellplatesand,after24hrs,treatedwithNMDI14for0,24,48and72hrs.ThecellsarecollectedandviablecellsarecountedbyusingtheCountessAutomatedCellCounter[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AksitMA,BowlingAD,EvansTA,etal.DecreasedmRNAandproteinstabilityofW1282Xlimitsresponsetomodulatortherapy.JCystFibros.2019;18(5):606-613.[2].MartinL,etal.Identificationandcharacterizationofsmallmoleculesthatinhibitnonsense-mediatedRNAdecayandsuppressnonsensep53mutations.CancerRes.2014Jun1;74(11):3104-1McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor