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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-0646 (-)-JQ-1


(JQ-1;JQ1)
Structure Price and Availability of    (-)-JQ-1
United States
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5mg $99 In-stock Inquiry
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 Distributor In Japan:  フナコシ株式会社 www.funakoshi.co.jp    
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  • Data Sheet
  • Introduction
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(-)-JQ-1  M.Wt: 456.99
(-)-JQ-1  Formula: C23H25ClN4O2S
(-)-JQ-1  Solubility: DMSO >150 mg/mL; Water <1 mg/mL; Ethanol 125 mg/mL
(-)-JQ-1  Purity: >98%
(-)-JQ-1  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 1268524-71-5

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(-)-JQ-1, the stereoisomer (+)-JQ1, showed no significant interaction with any bromodomain; (+)-JQ1 is an inhibitor for the BET. IC50 value: Target: BET bromodomain The ()-JQ1 stereoisomer has no appreciable affinity to BET bromodomains, whereas enantiomerically pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively.

1 . Filippakopoulos, Panagis et al. Selective inhibition of BET bromodomains From Nature (London, United Kingdom) (2010), 468(7327), 1067-1073.
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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