Bomedemstat-hydrochloride-IMG-7289-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBomedemstathydrochlorideCat.No.:HY-109169BSynonyms:IMG-7289hydrochloride分?式:C??H??ClFN?O?分?量:556.07作?靶點:HistoneDemethylase;Apoptosis作?通路:Epigenetics;Apoptosis儲存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(449.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7983mL8.9917mL17.9833mL5mM0.3597mL1.7983mL3.5967mL10mM0.1798mL0.8992mL1.7983mL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(fù)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(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性Bomedemstat(IMG-7289)hydrochloride?種具有?服活性和不可逆的lysine-specificdemethylase1(LSD1)抑制劑。Bomedemstathydrochloride可以增加H3K4和H3K9的甲化，然后改變因表達。Bomedemstathydrochloride具有抗癌活性，可抑制癌細胞增殖并誘導(dǎo)細胞凋亡。體外研究BomedemstatselectivelyinhibitsproliferationandinducesapoptosisofJak2V617Fcellsbyconcomitantlyincreasingexpressionandmethylationofp53[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBomedemstat(50nM-1μM;96h)enhancessurvival,inducesapoptosisviaBCL-XLandPUMAinaTP53-dependentmanner,andleadstocellcyclearrest[1].ApoptosisAnalysis[1]CellLine:SET-2cellsConcentration:50nM,100nM,and1μMIncubationTime:96hoursResult:DecreasedlevelsoftheantiapoptoticproteinBCL-XLandincreasedlevelsofthepro-apoptoticproteinPUMA.體內(nèi)研究Bomedemstattreatment(oralgavage;45mg/kg;oncedaily;56d)normalizesorimprovesbloodcellcounts,reducesspleenvolumes,restoresnormalsplenicarchitecture,andreducesbonemarrowfibrosis[1].AnimalModel:Mx-Jak2V617Fmice[1]Dosage:45mg/kgAdministration:Oralgavage;45mg/kg;oncedaily;56daysResult:Reducedsplenomegalysignificantlywithafewtreatedmicenormalizingtheirspleenweight,the56-daycourseledtopartialrestorationoflymphfolliclesandspleenarchitecturebyhistologicalexamination.REFERENCES[1].JonasSJutzi,etal.LSD1InhibitionProlongsSurvivalinMouseModelsofMPNbySelectivelyTargetingtheDiseaseClone.Hemasphere.2018Jun8;2(3):e54.[2].YuanFang,etal.LSD1/KDM1Ainhibitorsinclinicaltrials:advancesandprospects.JHematolOncol.2019Dec4;12(1):129.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese