(+)-JQ1

Cat. No. 4499

(+)-JQ1 C23H25ClN4O2S [1268524-70-4]

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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.

Licensing Information

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.

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Herrmann et al (2012) Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Oncotarget. [Epub ahead of print] 3 1588. PMID: 23249862.

Matzuk et al (2012) Small-molecule inhibition of BRDT for male contraception. Cell 150 673. PMID: 22901802.

Filippakopoulos et al (2010) Selective inhibition of BET bromodomains. Nature 468 1067. PMID: 20871596.

If you know of a relevant reference for (+)-JQ1 please let us know.

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

Perry et al (2015) BET bromodomains regulate transforming growth factor-β-induced proliferation and cytokine release in asthmatic airway smooth muscle. Nat Commun 290 9111. PMID: 25697361.

Do you know of a great paper that uses (+)-JQ1 from Tocris? If so please let us know.

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Keywords: (+)-JQ1, supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, Tocris Bioscience, Bromodomain Inhibitor products

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