dBET1

dBET1

CAT N°: 18044
Price:

From 66.00 56.10

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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (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
  • Correlated keywords
    • JQ-1 JQ1 lenalidomide bromodomain BET transcriptional activator proteasomal degradation phthalimides cereblon E3 leukemia PROTAC proteolysis target chimera
  • Product Overview:
    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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