A hetero-bifunctional molecule composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety; actively recruits BRD4 to cereblon

ARV-825 – 5 mg

Brand:
Cayman
CAS:
1818885-28-7
Storage:
-20
UN-No:
Non-Hazardous - /

ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}  

 

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Description

A hetero-bifunctional molecule composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety; actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at < 1 nM)

Formal name: 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide

Synonyms: 

Molecular weight: 923.4

CAS: 1818885-28-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|PROTACs||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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