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

Signaling Pathway



(JQ-1; JQ1)

(-)-JQ-1 Chemical Structure

(-)-JQ-1, the stereoisomer (+)-JQ1, showed no significant interaction with any bromodomain; (+)-JQ1 is an inhibitor for the BET.

Price and Availability of (-)-JQ-1
Size Price Stock
5 mg $99 In-stock
25 mg $429 In-stock
100 mg $715 In-stock
>1000 mg Get quote
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(-)-JQ-1 Data Sheet

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Cell Cycle/DNA Damage

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Biological Activity of (-)-JQ-1

(±)-JQ1 displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains. 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.

References on (-)-JQ-1

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

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

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