CellpenetrantProteolysisTargetingChimera(PROTAC)compoundbasedon(+)-JQ1conjugatedtoavonHippel-Lindau(VHL)ligand.RetainshighaffinityforBRD2,BRD3andBRD4bromodomains(Kd=13-60nM)butinducespreferentialdegradationofBRD4overBRD2andBRD3(DC50valuesfordegradationofBRD4are8and23nMinH661andH838cells,respectively).Exhibitspotentcytotoxicityandanti-proliferativeeffectsinAMLcelllines(pEC50=7.6inMv4-11cells).
Application
JQ1basedPROTACthatselectivelydegradesBRD4incells
ProductInformation
Purity: >98.0%
MW: 1002.64
Formula: C49H60ClN9O8S2
CASNo. 1797406-69-9
PhysicalState: Lyophilizedwhitetooff-whitesolid
Quantity: 1mg;5mg
Solubility: 100mg/mLinDMSO;or100mg/mlinethanol
Storage: Storedesiccatedassuppliedat-20°Cforupto3years.Storesolutionsat-80°Cforupto6monthsor-20°Cforupto1month.
Documents
References
1. Zengerleetal(2015)SelectivesmallmoleculeinduceddegradationoftheBETbromodomainproteinBRD4.ACS.Chem.Biol101770PMID: 26035625
2. Gaddetal(2017)StructuralbasisofPROTACcooperativerecognitionforselectiveproteindegradation.Nat.Chem.Biol.PMID: 28288108
3. Wurzetal(2017)A"clickchemistryplatform"fortherapidsynthesisofbispecificmoleculesforinducingproteindegradation.J.Med.Chem.PMID: 28378579
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那糖酵解中依赖NAD的酶不是要在线粒体内反应?
蛋白酶分布广泛,主要存在于人和动物消化道中,而消化道通过口与肛门与外界相通,属于外环境或外界环境
(溶菌酶、凝血酶原等)分布在内环境
(消化)酶分布在消化道

