JNJ-64619178-Onametostat-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJNJ-64619178Cat.No.:HY-101564CASNo.:2086772-26-9Synonyms:Onametostat分?式:C??H??BrN?O?分?量:483.36作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics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:125mg/mL(258.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0689mL10.3443mL20.6885mL5mM0.4138mL2.0689mL4.1377mL10mM0.2069mL1.0344mL2.0689mL請(qǐng)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(qǐng)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(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)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:≥2.08mg/mL(4.30mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.30mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性JNJ-64619178(Onametostat)?種偽不可逆的、?服活性的、選擇性蛋?精氨酸甲轉(zhuǎn)移酶5(PRMT5)抑制劑，IC50為0.14nM。JNJ-64619178有潛??于肺癌的研究。IC50&TargetIC50:0.14nM(PRMT5)[2]體外研究JNJ-64619178bindssimultaneouslytotheS-adenosylmethionine(SAM)-andproteinsubstrate-bindingpocketsofthePRMT5/MEP50complexwithapseudo-irreversiblemode-of-action.JNJ-64619178showspotentandbroadinhibitionofcellulargrowth[1].體內(nèi)研究OraladministrationofJNJ-64619178resultsinefficientinhibitionofdimethylationofSMD1/3proteins,componentsofthesplicingmachineryanddirectsubstratesofthemethylosome,inseveralnon-smallcelllungcancerandsmallcelllungcancercancermousexenograftmodels[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?UniversityofMunich.Fakult?tfürMedizin.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