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(+)-JQ1

4499 12 Citations Datasheet / COA / SDS
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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 (12)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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 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:

Product Datasheets

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Citations for (+)-JQ1

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

12 Citations: Showing 1 - 10

  1. 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
  2. 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
  3. 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
  4. Bromodomain protein BRD4 inhibitor JQ1 regulates potential prognostic molecules in advanced renal cell carcinoma.
    Authors: Sakaguchi
    Oncotarget  2018;9(33):23003
  5. 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
  6. IRE1α RNase-dependent lipid homeostasis promotes survival in Myc-transformed cancers.
    Authors: Xie Et al.
    J Clin Invest  2018;128:1300
  7. VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis.
    Authors: Chen
    Nat Commun  2017;8(1):383
  8. 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
  9. 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
  10. Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains.
    Authors: Shao Et al.
    Cell Rep  2016;16:3138

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