(+)-JQ1

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(+)-JQ1 | CAS No. 1268524-70-4 | Bromodomain Inhibitors
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Description: Potent and selective BET bromodomain inhibitor; cell permeable

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

Purity: ≥98%

Product Details
Citations (23)
Reviews

Biological Activity

(+)-JQ1 is a 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). (+)-JQ1 induces squamous differentiation in NUT midline carcinoma (NMC) cell lines and inhibits tumor growth in NMC xenograft models in vivo. (+)-JQ1 inhibits proliferation and induces autophagy in bladder cancer cells in vitro and in vivo. It also suppresses MYC gene expression and inhibits proliferation of lymphoma and leukemia cell lines. In human pulmonary microvasular endothelial cells (HPMEC), NF-κB activation, IL-6 and IL-8 expression and proliferation are inhibited by (+)-JQ1. The compound also inhibits transcription of ACE2 and TMPRSS2 genes in mouse lung tissue and prevents infection by SARS-CoV-2. In germ cells from male mice, (+)-JQ1 exhibits reversible contraceptive effects. (+)-JQ1 inhibits the BRD4-JUN-CCL2-TNF-α axis in pancreatic cancer cells and improves survival by reducing macrophage recruitment.

Inactive Analog also available.

Carboxylic acid-functionalized (Cat. No. 6588) and click-activated (alkyne) (Cat. No. 6589) versions for PROTAC development also 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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. Targeting MYC dependence in cancer by inhibiting BET bromodomains.
    Mertz JA, Conery AR, Bryant BM et al.
    Proc Natl Acad Sci U S A
  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
  4. Small-molecule inhibition of BRDT for male contraception.
    Matzuk et al.
    Cell, 2012;150:673

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Citations for (+)-JQ1

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

23 Citations: Showing 1 - 10

  1. Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL.
    Authors: Christopher J Et al.
    Cancer Res  2022;82:3375-3393
  2. BET and CDK Inhibition Reveal Differences in the Proliferation Control of Sympathetic Ganglion Neuroblasts and Adrenal Chromaffin Cells.
    Authors: Uwe Et al.
    Cancers (Basel)  2022;14
  3. BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4.
    Authors: Nasun Et al.
    Proc Natl Acad Sci U S A  2022;119
  4. TNF stimulation primarily modulates transcriptional burst size of NF-κB-regulated genes.
    Authors: Suzanne Et al.
    Mol Syst Biol  2021;17:e10127
  5. Transcriptional super-enhancers control cancer stemness and metastasis genes in squamous cell carcinoma.
    Authors: Yang Et al.
    Nat Commun  2021;12:3974
  6. Resistance to BET inhibitors in lung adenocarcinoma is mediated by casein kinase phosphorylation of BRD4.
    Authors: Daniel Et al.
    Oncogenesis  2021;10:27
  7. BET-Inhibitor I-BET762 and PARP-Inhibitor Talazoparib Synergy in Small Cell Lung Cancer Cells.
    Authors: Francesco Paolo Et al.
    Int J Mol Sci  2020;21
  8. BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response.
    Authors: Andrieu Et al.
    Cancer Lett  2019;465:45
  9. Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer.
    Authors: Noblejas-Lopez Et al.
    J Exp Clin Cancer Res  2019;38:383
  10. Super-Enhancer-Associated LncRNA UCA1 Interacts Directly with AMOT to Activate YAP Target Genes in Epithelial Ovarian Cancer.
    Authors: Lin Et al.
    iScience  2019;17:242
  11. Bromodomain protein BRD4 inhibitor JQ1 regulates potential prognostic molecules in advanced renal cell carcinoma.
    Authors: Sakaguchi
    Oncotarget  2018;9(33):23003
  12. PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells.
    Authors: Georgilis Et al.
    Cancer Cell  2018;34:85
  13. Targeting the HTLV-I-Regulated BATF3/IRF4 Transcriptional Network in Adult T Cell Leukemia/Lymphoma.
    Authors: Michiyuki Et al.
    Cancer Cell  2018;34:286-297.e10
  14. IRE1α RNase-dependent lipid homeostasis promotes survival in Myc-transformed cancers.
    Authors: Xie Et al.
    J Clin Invest  2018;128:1300
  15. VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis.
    Authors: Chen
    Nat Commun  2017;8(1):383
  16. The Short Isoform of BRD4 Promotes HIV-1 Latency by Engaging Repressive SWI/SNF Chromatin-Remodeling Complexes.
    Authors: Qiang Et al.
    Mol Cell  2017;67:1001-1012.e6
  17. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function.
    Authors: Scott W Et al.
    Mol Cell  2017;66:517-532.e9
  18. AMPK-ULK1-Mediated Autophagy Confers Resistance to BET Inhibitor JQ1 in Acute Myeloid Leukemia Stem Cells.
    Authors: Jang Et al.
    Clin Cancer Res  2017;23:2781
  19. MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells.
    Authors: Kato Et al.
    Oncotarget  2016;7:77378
  20. Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains.
    Authors: Shao Et al.
    Cell Rep  2016;16:3138
  21. Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity.
    Authors: Sartor Et al.
    J Neurosci  2015;35:15062
  22. 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
  23. Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement.
    Authors: Robert Et al.
    Breast Cancer Res Treat  2015;150:265-78

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