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LifeSensors/PC1001 MZ1 5mg/PC1001 MZ1 5mg

CellpenetrantProteolysisTargetingChimera(PROTAC)compoundbasedon (+)-JQ1 conjugatedtoavonHippel-Lindau(VHL)ligand.RetainshighaffinityforBRD2,BRD3andBRD4bromodomains(Kd =13-60nM)butinducespreferentialdegradationofBRD4overBRD2andBRD3(DC50 valuesfordegradationofBRD4are8and23nMinH661andH838cells,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.    Zengerle etal (2015)SelectivesmallmoleculeinduceddegradationoftheBETbromodomainproteinBRD4.ACS.Chem.Biol 10 1770PMID: 26035625

2.    Gadd etal (2017)StructuralbasisofPROTACcooperativerecognitionforselectiveproteindegradation.Nat.Chem.Biol.PMID: 28288108

3.    Wurz etal (2017)A"Clickchemistryplatform"fortherapidsynthesisofbispecificmoleculesforinducingproteindegradation.J.Med.Chem.PMID: 28378579

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