Displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains; binds BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM

(+)-JQ1 – 5 mg

Brand:
Cayman
CAS:
1268524-70-4
Storage:
-20
UN-No:
Non-Hazardous - /

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. JQ1 displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains.{19044,28490} Enantiomerically pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM, respectively, whereas the (−)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains.{19044} JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.{19044,28490,20263,20272,20182} See the Structural Genomics Consortium (SGC) website for more information.  

 

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SKU: 11187 - 5 mg Category:

Description

Displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains; binds BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM, respectively

Formal name: (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 1,1-dimethylethyl ester

Synonyms: 

Molecular weight: 457

CAS: 1268524-70-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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