JNJ-64619178-Onametostat-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJNJ-64619178Cat.No.:HY-101564CASNo.:2086772-26-9Synonyms:Onametostat分⼦式:C₂₂H₂₃BrN₆O₂分⼦量:483.36作⽤靶点:HistoneMethyltransferase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:125mg/mL(258.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0689mL10.3443mL20.6885mL5mM0.4138mL2.0689mL4.1377mL10mM0.2069mL1.0344mL2.0689mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.30mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.30mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.30mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JNJ-64619178(Onametostat)⼀种伪不可逆的、⼝服活性的、选择性蛋⽩精氨酸甲转移酶5(PRMT5)抑制剂，IC50为0.14nM。JNJ-64619178有潜⼒⽤于肺癌的研究。IC50&TargetIC50:0.14nM(PRMT5)[2]体外研究JNJ-64619178bindssimultaneouslytotheS-adenosylmethionine(SAM)-andproteinsubstrate-bindingpocketsofthePRMT5/MEP50complexwithapseudo-irreversiblemode-of-action.JNJ-64619178showspotentandbroadinhibitionofcellulargrowth[1].体内研究OraladministrationofJNJ-64619178resultsinefficientinhibitionofdimethylationofSMD1/3proteins,componentsofthesplicingmachineryanddirectsubstratesofthemethylosome,inseveralnon-smallcelllungcancerandsmallcelllungcancercancermousexenograftmodels[1].户使⽤本产品发表的科研⽂献•UniversityofMunich.FakultätfürMedizin.2022Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TongfeiWu,etal.Abstract4859:JNJ-64619178,aselectiveandpseudo-irreversiblePRMT5inhibitorwithpotentinvitroandinvivoactivity,demonstratedinseverallungcancermodels.[2].TaoH,etal.DiscoveryofNovelPRMT5InhibitorsbyVirtualScreeningandBiologicalEvaluations.ChemPharmBull(Tokyo).2019;67(4):382-388.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese