(+)-JQ1

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Cat.No. 4499 - (+)-JQ1 | C23H25ClN4O2S | CAS No. 1268524-70-4
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% (HPLC)
Datasheet
Citations (12)
Reviews (2)
Literature (5)

Biological Activity for (+)-JQ1

(+)-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). 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.

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 for (+)-JQ1

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.

Compound Libraries for (+)-JQ1

(+)-JQ1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for (+)-JQ1

M. Wt 456.99
Formula C23H25ClN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1268524-70-4
PubChem ID 46907787
InChI Key DNVXATUJJDPFDM-KRWDZBQOSA-N
Smiles O=C(OC(C)(C)C)C[C@@H]1N=C(C4=CC=C(Cl)C=C4)C3=C(SC(C)=C3C)N2C1=NN=C2C

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.

Solubility Data for (+)-JQ1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.7 100
ethanol 45.7 100

Preparing Stock Solutions for (+)-JQ1

The following data is based on the product molecular weight 456.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.94 mL 21.88 mL
5 mM 0.44 mL 2.19 mL 4.38 mL
10 mM 0.22 mL 1.09 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets for (+)-JQ1

Certificate of Analysis / Product Datasheet
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References for (+)-JQ1

References are publications that support the biological activity of the product.

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

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


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

View Related Products by Target

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View all Bromodomain Inhibitors

Keywords: (+)-JQ1, (+)-JQ1 supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, Bromodomains, 4499, Tocris Bioscience

12 Citations for (+)-JQ1

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

Noblejas-Lopez et al (2019) Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. J Exp Clin Cancer Res 38 383 PMID: 31470872

Shao et al (2016) Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep 16 3138 PMID: 27653680

Kato et al (2016) MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells. Oncotarget 7 77378 PMID: 27764802

Andrieu et al (2019) BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response. Cancer Lett 465 45 PMID: 31473251


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Reviews for (+)-JQ1

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Works good.
By Anonymous on 06/22/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: U2OS

JQ1 (1 μM)

PMID: 30463005
review image

Reprogramming media with JQ1.
By Anonymous on 02/23/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: ipsc

500 nM

PMID: 27653680
review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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