(+)-JQ1

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; K_d 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

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

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. VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis
   J Chen, Y Fu, DS Day, Y Sun, S Wang, X Liang, F Gu, F Zhang, SM Stevens, P Zhou, K Li, Y Zhang, RZ Lin, LEH Smith, J Zhang, K Sun, JM Melero-Mar, Z Han, PJ Park, B Zhang, WT Pu
   Nat Commun, 2017;8(1):383.
3. BET bromodomains regulate transforming growth factor-beta-induced proliferation and cytokine release in asthmatic airway smooth muscle.
   Perry M, Durham A, Austin P, Adcock I, Chung K
   J Biol Chem, 2015;290(14):9111-21.
4. Selective inhibition of BET bromodomains.
   Filippakopoulos et al.
   Nature, 2010;468:1067
5. 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
6. Small-molecule inhibition of BRDT for male contraception.
   Matzuk et al.
   Cell, 2012;150:673

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