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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% (HPLC)
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). (+)-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.
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 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.
| 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
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 3 1588 PMID: 23249862
Matzuk et al (2012) Small-molecule inhibition of BRDT for male contraception. Cell 150 673 PMID: 22901802
Li et al (2019) BET inhibitor JQ1 suppresses cell proliferation via inducing autophagy and activating LKB1/AMPK in bladder cancer cells. Cancer Med. 8 4792 PMID: 31250978
Mumby et al (2017) Bromodomain and extra-terminal protein mimic JQ1 decreases inflammation in human vascular endothelial cells: Implications for pulmonary arterial hypertension. Respirology 22 157 PMID: 27539364
Qiao et al (2020) Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2. Proc.Natl.Acad.Sci.U.S.A. 118 e2021450118 PMID: 33310900
Mertz et al (2011) Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc.Natl.Acad.Sci.U.S.A. 108 16669 PMID: 21949397
Tu et al (2021) TNF-a-producing macrophages determine subtype identity and prognosis via AP1 enhancer reprogramming in pancreatic cancer. Nat.Cancer 2 1185 PMID: 35122059
If you know of a relevant reference for (+)-JQ1, please let us know.
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Keywords: (+)-JQ1, (+)-JQ1 supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, autophagy, induces, activators, activates, induction, anti-inflammatory, coronavirus, SARS-CoV-2, Bromodomains, Coronavirus, 4499, Tocris Bioscience
23 Citations for (+)-JQ1
Citations are publications that use Tocris products. Selected citations for (+)-JQ1 include:
Georgilis et al (2018) PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells. Cancer Cell 34 85 PMID: 29990503
Xie et al (2018) IRE1α RNase-dependent lipid homeostasis promotes survival in Myc-transformed cancers. J Clin Invest 128 1300 PMID: 29381485
Chen (2017) VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis. Nat Commun 8 383 PMID: 28851877
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
Yang et al (2021) Transcriptional super-enhancers control cancer stemness and metastasis genes in squamous cell carcinoma. Nat Commun 12 3974 PMID: 34172737
Suzanne et al (2021) TNF stimulation primarily modulates transcriptional burst size of NF-κB-regulated genes. Mol Syst Biol 17 e10127 PMID: 34288498
Daniel et al (2021) Resistance to BET inhibitors in lung adenocarcinoma is mediated by casein kinase phosphorylation of BRD4. Oncogenesis 10 27 PMID: 33712563
Lin et al (2019) Super-Enhancer-Associated LncRNA UCA1 Interacts Directly with AMOT to Activate YAP Target Genes in Epithelial Ovarian Cancer. iScience 17 242 PMID: 31307004
Robert et al (2015) Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement. Breast Cancer Res Treat 150 265-78 PMID: 25721606
Sartor et al (2015) Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity. J Neurosci 35 15062 PMID: 26558777
Michiyuki et al (2018) Targeting the HTLV-I-Regulated BATF3/IRF4 Transcriptional Network in Adult T Cell Leukemia/Lymphoma. Cancer Cell 34 286-297.e10 PMID: 30057145
Scott W et al (2017) Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and Lysosomal Function. Mol Cell 66 517-532.e9 PMID: 28525743
Qiang et al (2017) The Short Isoform of BRD4 Promotes HIV-1 Latency by Engaging Repressive SWI/SNF Chromatin-Remodeling Complexes. Mol Cell 67 1001-1012.e6 PMID: 28844864
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
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
Sakaguchi (2018) Bromodomain protein BRD4 inhibitor JQ1 regulates potential prognostic molecules in advanced renal cell carcinoma. Oncotarget 9 23003 PMID: 29796168
Uwe et al (2022) BET and CDK Inhibition Reveal Differences in the Proliferation Control of Sympathetic Ganglion Neuroblasts and Adrenal Chromaffin Cells. Cancers (Basel) 14 PMID: 35681734
Nasun et al (2022) BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4. Proc Natl Acad Sci U S A 119 PMID: 34983841
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
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
Francesco Paolo et al (2020) BET-Inhibitor I-BET762 and PARP-Inhibitor Talazoparib Synergy in Small Cell Lung Cancer Cells. Int J Mol Sci 21 PMID: 33339368
Shao et al (2016) Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep 16 3138 PMID: 27653680
Jang et al (2017) AMPK-ULK1-Mediated Autophagy Confers Resistance to BET Inhibitor JQ1 in Acute Myeloid Leukemia Stem Cells. Clin Cancer Res 23 2781 PMID: 27864418
Do you know of a great paper that uses (+)-JQ1 from Tocris? Please let us know.
Reviews for (+)-JQ1
Average Rating: 5 (Based on 2 Reviews.)
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Filter by:
Works good.
By
Anonymous on 06/22/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: U2OS
JQ1 (1 μM)
Reprogramming media with JQ1.
By
Anonymous on 02/23/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: ipsc
500 nM
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