CAS No. : 1268524-71-5

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I001076
Synonyms:(R)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
Molecular Formula:C₂₃H₂₅ClN₄O₂S
Molecular Weight:456.99
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Appearance:A crystalline solid
Cat No:I001076
Cas No:1268524-71-5

(R)-(-)-JQ1 Enantiomer, the stereoisomer (+)-JQ1, showed no significant interaction with any bromodomain; (+)-JQ1 is an inhibitor for the BET.
IC50 value:
Target: BET bromodomain
The (R)-(-)-JQ1 Enantiomer 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. ...

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