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 ActivityPotent, 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 also available.
External Portal InformationChemicalprobes.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.
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.
Selective inhibition of BET bromodomains.
Filippakopoulos et al.
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
Small-molecule inhibition of BRDT for male contraception.
Matzuk et al.
Citations for (+)-JQ1
The citations listed below are publications that use Tocris products. Selected citations for (+)-JQ1 include:
5 Citations: Showing 1 - 5
Bromodomain protein BRD4 inhibitor JQ1 regulates potential prognostic molecules in advanced renal cell carcinoma.
VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis.
Nat Commun 2017;8(1):383
MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells.
Authors: Kato Et al.
Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity.
Authors: Sartor Et al.
J Neurosci 2015;35:15062
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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