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Home   »   Product Pathways  »  Cancer  »  (+)-JQ-1

Products are for research use only. Not for human use. We do not sell to patients.


CS-0581 (+)-JQ-1


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(+)-JQ-1  M.Wt: 456.99
(+)-JQ-1  Formula: C23H25ClN4O2S
(+)-JQ-1  Solubility: DMSO
(+)-JQ-1  Purity: >98%
(+)-JQ-1  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 1268524-70-4

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(+)-JQ-1 is a BET bromodomains inhibitor

1 . Selective inhibition of BET bromodomains By Filippakopoulos, Panagis; Qi, Jun; Picaud, Sarah; Shen, Yao; Smith, William B.; Fedorov, Oleg; Morse, Elizabeth M.; Keates, Tracey; Hickman, Tyler T.; Felletar, Ildiko; et al From Nature. 2010 Dec 23;468(7327):1067-73. Epub 2010 Sep 24.
Abstract
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described. Here we report a cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains. High potency and specificity towards a subset of human bromodomains is explained by co-crystal structures with bromodomain and extra-terminal (BET) family member BRD4, revealing excellent shape complementarity with the acetyl-lysine binding cavity. Recurrent translocation of BRD4 is observed in a genetically-defined, incurable subtype of human squamous carcinoma. Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models. ...

BET bromodomain  |  
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