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LifeSensors/PC1002 dBET1 10mg/PC1002 dBET1 10mg

dBET1isapotentandselectiveBRD4proteindegrader.Themolecule,dubbed“degronimid”,isharnessedbycombiningtwospecifichighaffinityproteinligands,(+)-JQ1forBRD4andPhthalimideforE3ubiquitinligasecereblon(CRBN),tetheredbyalinker.Fullyexploitingthecells’ownprotein-degrADIngmachinery,themoleculedragstheubiquitinligasecomplexintothetaggedprotein,leadingtoafast,sustainable,CRBN-dependentandligand-guidedBRD4degradation.Itissoselectivethatonlythreeproteins,BRD2,3,4,of>7000withinthecell,wereaffected.dBET1demonstratedpowerfulanti-leukemiaactivitiesbothincellandinanimalmodel,withfewnoticeablesideeffects.


Application

JQ1 basedPROTACthatselectivelydegradesBRD4incells


ProductInformation

Purity:                  >99.5% 

MW:                      799.7

Formula:               C38H37ClN8O7S∙0.8H2O

CASNo.                   1799711-21-9

PhysicalState:          Lyophilizedwhitepowder

Quantity:              5mg;10mg;25mg

Solubility:              40mg/mLinDMSO

Storage:                  Storedesiccatedassuppliedat-20°Cforupto3years.Storesolutionsat-80°Cforupto6monthsor-20°Cforupto1month.



Documents


References

1.    Winter etal (2015)DrugDevelopment.Phthalimideconjugationasastrategyfor invivo targetproteindegradation.Science 348 1376PMID: 25999370

2.    Wurz etal (2017)A"Clickchemistryplatform"fortherapidsynthesisofbispecificmoleculesforinducingproteindegradation.J.Med.Chem.10.1021PMID: 28378579


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