A hybrid molecule that combines (+)-JQ1 and thalidomide; induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice

dBET1 – 1 mg

Brand:
Cayman
CAS:
1799711-21-9
Storage:
-20
UN-No:
Non-Hazardous - /

dBET1 is a hybrid molecule that combines (+)-JQ1 (Item No. 11187) and thalidomide (Item No. 14610).{29054} The JQ1 portion facilitates binding of dBET1 to the bromodomains of BET family transcriptional activators. The thalidomide moiety drives proteasomal degradation, as phthalimides bind cereblon to create a substrate recognition site for E3 protein ligase complex-mediated ubiquitination. dBET1 induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice.  

 

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Description

A hybrid molecule that combines (+)-JQ1 and thalidomide; induces cereblon-dependent BET protein degradation in vitro (EC50 = 430 nM) and in vivo and delays leukemia progression in mice

Formal name: (6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

Synonyms: 

Molecular weight: 785.3

CAS: 1799711-21-9

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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