Catalog Number: 4499
Chemical 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
Biological Activity
Potent, high affinity, selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively). Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models in vivo. Exhibits reversible contraceptive effects in germ cells from male mice. Inactive analog (-)-JQ1 available.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of (+)-JQ1 is reviewed on the chemical probes website.
Technical Data
  • M.Wt:
    456.99
  • Formula:
    C23H25ClN4O2S
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1268524-70-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (+)-JQ1 probe summary on the SGC website.
Other Product-Specific Information:
Background References
  1. Small-molecule inhibition of BRDT for male contraception.
    Matzuk et al.
    Cell, 2012;150:673
  2. Selective inhibition of BET bromodomains.
    Filippakopoulos et al.
    Nature, 2010;468:1067
  3. Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.
    Herrmann et al.
    Oncotarget. [Epub ahead of print], 2012;3:1588
Citations:

The citations listed below are publications that use Tocris products. Selected citations for (+)-JQ1 include:

1 Citations: Showing 1 - 1

  1. BET bromodomains regulate transforming growth factor-β-induced proliferation and cytokine release in asthmatic airway smooth muscle.
    Authors: Perry Et al.
    Nat Commun 2015;290:9111

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