1268524-70-4 | (+)-JQ-1

Packsize	Purity	Availability	Price	Discounted Price
10mg	97%	in stock	$15.00	$10.00
25mg	97%	in stock	$25.00	$17.00
50mg	97%	in stock	$45.00	$31.00
100mg	97%	in stock	$51.00	$36.00
250mg	97%	in stock	$101.00	$71.00
500mg	97%	in stock	$188.00	$131.00
1g	97%	in stock	$238.00	$167.00
5g	97%	in stock	$836.00	$585.00
10g	97%	in stock	$1,415.00	$990.00

Description

• Catalog Number: AA37851
• Chemical Name: (+)-JQ-1
• CAS Number: 1268524-70-4
• Molecular Formula: C23H25ClN4O2S
• Molecular Weight: 456.9882
• MDL Number: MFCD22683748
• SMILES: O=C(OC(C)(C)C)C[C@@H]1N=C(c2ccc(cc2)Cl)c2c(-n3c1nnc3C)sc(c2C)C

Computed Properties

• Complexity: 706
• Covalently-Bonded Unit Count: 1
• Defined Atom Stereocenter Count: 1
• Heavy Atom Count: 31
• Hydrogen Bond Acceptor Count: 6
• Rotatable Bond Count: 5
• XLogP3: 4.9

Literature

• Selective gene dependencies in MYCN-amplified neuroblastoma include the core transcriptional regulatory circuitry.

  Nature genetics 20180901

• Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.

  The Journal of biological chemistry 20180216

• Inhibition of Bromodomain and Extraterminal Domain Family Proteins Ameliorates Experimental Renal Damage.

  Journal of the American Society of Nephrology : JASN 20170201

• Bromodomain and Extraterminal Protein Inhibitor JQ1 Suppresses Thyroid Tumor Growth in a Mouse Model.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20170115

• The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer.

  Oncogene 20170105

• Design and characterization of bivalent BET inhibitors.

  Nature chemical biology 20161201

• The BET-Bromodomain Inhibitor JQ1 Reduces Inflammation and Tau Phosphorylation at Ser396 in the Brain of the 3xTg Model of Alzheimer's Disease.

  Current Alzheimer research 20160901

• Antimyeloma activity of bromodomain inhibitors on the human myeloma cell line U266 by downregulation of MYCL.

  Anti-cancer drugs 20160901

• BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members.

  Molecular cancer therapeutics 20160901

• Loss of TRIM33 causes resistance to BET bromodomain inhibitors through MYC- and TGF-β-dependent mechanisms.

  Proceedings of the National Academy of Sciences of the United States of America 20160802

• In Silico Analysis Guides Selection of BET Inhibitors for Triple-Negative Breast Cancer Treatment.

  Molecular cancer therapeutics 20160801

• BET bromodomain inhibitors suppress EWS-FLI1-dependent transcription and the IGF1 autocrine mechanism in Ewing sarcoma.

  Oncotarget 20160712

• Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.

  Molecular cancer therapeutics 20160601

• Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice.

  Toxicology and applied pharmacology 20160601

• BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma.

  Cancer medicine 20160601

• Epigenetic reader BRD4 inhibition as a therapeutic strategy to suppress E2F2-cell cycle regulation circuit in liver cancer.

  Oncotarget 20160531

• The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression and Induce Anticancer Effects.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20160515

• The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma.

  Molecular cancer therapeutics 20160501

• BRD4 Regulates EZH2 Transcription through Upregulation of C-MYC and Represents a Novel Therapeutic Target in Bladder Cancer.

  Molecular cancer therapeutics 20160501

• Keap1-Independent Regulation of Nrf2 Activity by Protein Acetylation and a BET Bromodomain Protein.

  PLoS genetics 20160501

• Targeting the epigenetic readers in Ewing sarcoma inhibits the oncogenic transcription factor EWS/Fli1.

  Oncotarget 20160426

• Cancer Differentiating Agent Hexamethylene Bisacetamide Inhibits BET Bromodomain Proteins.

  Cancer research 20160415

• Inhibition of the acetyl lysine-binding pocket of bromodomain and extraterminal domain proteins interferes with adipogenesis.

  Biochemical and biophysical research communications 20160415

• MYC regulates the antitumor immune response through CD47 and PD-L1.

  Science (New York, N.Y.) 20160408

• MCM5 as a target of BET inhibitors in thyroid cancer cells.

  Endocrine-related cancer 20160401

• Inhibition of MUC1-C Suppresses MYC Expression and Attenuates Malignant Growth in KRAS Mutant Lung Adenocarcinomas.

  Cancer research 20160315

• The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models.

  Oncogene 20160218

• Dual mTOR inhibitor MLN0128 suppresses Merkel cell carcinoma (MCC) xenograft tumor growth.

  Oncotarget 20160209

• Bromodomain and extraterminal (BET) proteins regulate biliary-driven liver regeneration.

  Journal of hepatology 20160201

• CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer.

  The Journal of clinical investigation 20160201

• Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer.

  Nature 20160121

• Suppression of BRD4 inhibits human hepatocellular carcinoma by repressing MYC and enhancing BIM expression.

  Oncotarget 20160119

• Inhibition of BRD4 suppresses tumor growth and enhances iodine uptake in thyroid cancer.

  Biochemical and biophysical research communications 20160115

• Targeting the EWS-ETS transcriptional program by BET bromodomain inhibition in Ewing sarcoma.

  Oncotarget 20160112

• Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase-dependent NF-κB activation in rheumatoid fibroblast-like synoviocytes.

  Rheumatology (Oxford, England) 20160101

• BET protein inhibitor JQ1 inhibits growth and modulates WNT signaling in mesenchymal stem cells.

  Stem cell research & therapy 20160101

• BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1.

  Theranostics 20160101

• BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell.

  PloS one 20160101

• BET Bromodomain Suppression Inhibits VEGF-induced Angiogenesis and Vascular Permeability by Blocking VEGFR2-mediated Activation of PAK1 and eNOS.

  Scientific reports 20160101

• BRD4 is a novel therapeutic target for liver fibrosis.

  Proceedings of the National Academy of Sciences of the United States of America 20151222

• Therapeutic targeting of BET protein BRD4 delays murine lupus.

  International immunopharmacology 20151201

• Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20151111

• The BET bromodomain inhibitor, JQ1, facilitates c-FLIP degradation and enhances TRAIL-induced apoptosis independent of BRD4 and c-Myc inhibition.

  Oncotarget 20151027

• Induction of USP17 by combining BET and HDAC inhibitors in breast cancer cells.

  Oncotarget 20151020

• BRD4-targeted therapy induces Myc-independent cytotoxicity in Gnaq/11-mutatant uveal melanoma cells.

  Oncotarget 20151020

• EGFR Mutation Promotes Glioblastoma through Epigenome and Transcription Factor Network Remodeling.

  Molecular cell 20151015

• Sensitivity of Small Cell Lung Cancer to BET Inhibition Is Mediated by Regulation of ASCL1 Gene Expression.

  Molecular cancer therapeutics 20151001

• BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice.

  Nature neuroscience 20151001

• Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma.

  Nature medicine 20151001

• Complete hematologic response of early T-cell progenitor acute lymphoblastic leukemia to the γ-secretase inhibitor BMS-906024: genetic and epigenetic findings in an outlier case.

  Cold Spring Harbor molecular case studies 20151001

• Inhibition of Super-Enhancer Activity in Autoinflammatory Site-Derived T Cells Reduces Disease-Associated Gene Expression.

  Cell reports 20150929

• Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib.

  Blood 20150924

• BET inhibitor resistance emerges from leukaemia stem cells.

  Nature 20150924

• Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6.

  Nucleic acids research 20150918

• Bromodomain and extraterminal inhibition blocks tumor progression and promotes differentiation in neuroblastoma.

  Surgery 20150901

• Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.

  Pharmacological research 20150901

• BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.

  Chembiochem : a European journal of chemical biology 20150901

• Bromodomain-Containing Protein 4: The Epigenetic Origin of Pulmonary Arterial Hypertension.

  Circulation research 20150828

• CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.

  Proceedings of the National Academy of Sciences of the United States of America 20150825

• Carbonic anhydrase IX induction defines a heterogeneous cancer cell response to hypoxia and mediates stem cell-like properties and sensitivity to HDAC inhibition.

  Oncotarget 20150814

• Therapeutic targeting of BET bromodomain protein, Brd4, delays cyst growth in ADPKD.

  Human molecular genetics 20150715

• Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies.

  Nucleic acids research 20150713

• BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells.

  Oncotarget 20150710

• Synergistic induction of cell death in haematological malignancies by combined phosphoinositide-3-kinase and BET bromodomain inhibition.

  British journal of haematology 20150701

• Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion.

  Oncotarget 20150630

• BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia.

  Molecular cell 20150618

• Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

  Chemistry & biology 20150618

• A Cre-conditional MYCN-driven neuroblastoma mouse model as an improved tool for preclinical studies.

  Oncogene 20150601

• Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma.

  International journal of cancer 20150501

• BET bromodomain inhibition suppresses graft-versus-host disease after allogeneic bone marrow transplantation in mice.

  Blood 20150423

• Deacetylase inhibitors repress STAT5-mediated transcription by interfering with bromodomain and extra-terminal (BET) protein function.

  Nucleic acids research 20150420

• Nanog requires BRD4 to maintain murine embryonic stem cell pluripotency and is suppressed by bromodomain inhibitor JQ1 together with Lefty1.

  Stem cells and development 20150401

• Inhibition of BET proteins impairs estrogen-mediated growth and transcription in breast cancers by pausing RNA polymerase advancement.

  Breast cancer research and treatment 20150401

• Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturation.

  Journal of immunology (Baltimore, Md. : 1950) 20150401

• [Mechanism of Notch1 Pathway in SUP-B15 Cell Apoptosis Induced by JQ1].

  Zhongguo shi yan xue ye xue za zhi 20150401

• JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer.

  Oncotarget 20150330

• The MZF1/c-MYC axis mediates lung adenocarcinoma progression caused by wild-type lkb1 loss.

  Oncogene 20150326

• BRAD4 plays a critical role in germinal center response by regulating Bcl-6 and NF-κB activation.

  Cellular immunology 20150301

• Epstein-Barr virus oncoprotein super-enhancers control B cell growth.

  Cell host & microbe 20150211

• Bromodomain inhibition by JQ1 suppresses lipopolysaccharide-stimulated interleukin-6 secretion in multiple myeloma cells.

  Cytokine 20150201

• Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers.

  Oncotarget 20150201

• An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma.

  Proceedings of the National Academy of Sciences of the United States of America 20150106

• Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20150101

• GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1.

  Scientific reports 20150101

• RNA sequencing reveals distinct mechanisms underlying BET inhibitor JQ1-mediated modulation of the LPS-induced activation of BV-2 microglial cells.

  Journal of neuroinflammation 20150101

• BET inhibitors induce apoptosis through a MYC independent mechanism and synergise with CDK inhibitors to kill osteosarcoma cells.

  Scientific reports 20150101

• Direct and indirect targeting of MYC to treat acute myeloid leukemia.

  Cancer chemotherapy and pharmacology 20150101

• Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells.

  eLife 20150101

• Dual transcriptome sequencing reveals resistance of TLR4 ligand-activated bone marrow-derived macrophages to inflammation mediated by the BET inhibitor JQ1.

  Scientific reports 20150101

• Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth.

  Drug design, development and therapy 20150101

• BET protein inhibitor JQ1 attenuates Myc-amplified MCC tumor growth in vivo.

  Cancer research 20141201

• BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones.

  Nature structural & molecular biology 20141201

• Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

  Science (New York, N.Y.) 20141031

• NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis.

  Molecular cell 20141023

• PRC2 loss amplifies Ras-driven transcription and confers sensitivity to BRD4-based therapies.

  Nature 20141009

• BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD.

  Molecular cancer therapeutics 20141001

• Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.

  Proceedings of the National Academy of Sciences of the United States of America 20140805

• 'Minimalist' cyclopropene-containing photo-cross-linkers suitable for live-cell imaging and affinity-based protein labeling.

  Journal of the American Chemical Society 20140716

• Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis.

  Cellular signalling 20140701

• BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction.

  Journal of dental research 20140701

• An epigenomic approach to therapy for tamoxifen-resistant breast cancer.

  Cell research 20140701

• Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.

  Nature medicine 20140701

• Activation of SOX2 expression by BRD4-NUT oncogenic fusion drives neoplastic transformation in NUT midline carcinoma.

  Cancer research 20140615

• Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.

  Nature 20140612

• Histone deacetylase 2 and N-Myc reduce p53 protein phosphorylation at serine 46 by repressing gene transcription of tumor protein 53-induced nuclear protein 1.

  Oncotarget 20140601

• Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors.

  Oncogene 20140529

• Bromodomain and extraterminal proteins suppress NF-E2-related factor 2-mediated antioxidant gene expression.

  Journal of immunology (Baltimore, Md. : 1950) 20140515

• MLL3 is a haploinsufficient 7q tumor suppressor in acute myeloid leukemia.

  Cancer cell 20140512

• Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA.

  Oncogene 20140501

• Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells.

  Molecular cancer therapeutics 20140501

• Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2.

  Molecular cancer therapeutics 20140501

• Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma.

  Oncotarget 20140501

• Therapeutic targeting of c-Myc in T-cell acute lymphoblastic leukemia, T-ALL.

  Oncotarget 20140501

• The bromodomain protein BRD4 regulates the KEAP1/NRF2-dependent oxidative stress response.

  Cell death & disease 20140401

• Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.

  The Journal of biological chemistry 20140328

• Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle.

  Nature communications 20140319

• The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis.

  Journal of leukocyte biology 20140301

• BET bromodomain inhibition of MYC-amplified medulloblastoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20140215

• c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells.

  Blood 20140213

• Regulation of MYC expression and differential JQ1 sensitivity in cancer cells.

  PloS one 20140101

• Brd4 is essential for IL-1β-induced inflammation in human airway epithelial cells.

  PloS one 20140101

• The histone deacetylase Hdac1 regulates inflammatory signalling in intestinal epithelial cells.

  Journal of inflammation (London, England) 20140101

• Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma.

  Cancer cell 20131209

• Disruption of the MYC-miRNA-EZH2 loop to suppress aggressive B-cell lymphoma survival and clonogenicity.

  Leukemia 20131201

• BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.

  Cancer medicine 20131201

• Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20131115

• BET bromodomain protein inhibition is a therapeutic option for medulloblastoma.

  Oncotarget 20131101

• BET acetyl-lysine binding proteins control pathological cardiac hypertrophy.

  Journal of molecular and cellular cardiology 20131001

• Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

  ACS medicinal chemistry letters 20130912

• Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis.

  The American journal of pathology 20130801

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

  Bioorganic & medicinal chemistry letters 20130801

• Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers.

  EMBO molecular medicine 20130801

• BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia.

  Blood cancer journal 20130701

• BRD4 coordinates recruitment of pause release factor P-TEFb and the pausing complex NELF/DSIF to regulate transcription elongation of interferon-stimulated genes.

  Molecular and cellular biology 20130601

• The methyltransferase SMYD3 mediates the recruitment of transcriptional cofactors at the myostatin and c-Met genes and regulates skeletal muscle atrophy.

  Genes & development 20130601

• Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

  Journal of medicinal chemistry 20130425

• Selective inhibition of tumor oncogenes by disruption of super-enhancers.

  Cell 20130411

• Inhibition of BET bromodomain targets genetically diverse glioblastoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20130401

• BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.

  Journal of immunology (Baltimore, Md. : 1950) 20130401

• Targeting MYCN in neuroblastoma by BET bromodomain inhibition.

  Cancer discovery 20130301

• Androgen receptor promotes ligand-independent prostate cancer progression through c-Myc upregulation.

  PloS one 20130101

• Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells.

  The Journal of biological chemistry 20121214

• BET bromodomain inhibition as a novel strategy for reactivation of HIV-1.

  Journal of leukocyte biology 20121201

• Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins.

  Proceedings of the National Academy of Sciences of the United States of America 20121120

• Reactivation of latent HIV-1 by inhibition of BRD4.

  Cell reports 20121025

• Bromodomain and extra-terminal (BET) bromodomain inhibition activate transcription via transient release of positive transcription elongation factor b (P-TEFb) from 7SK small nuclear ribonucleoprotein.

  The Journal of biological chemistry 20121019

• BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.

  Blood 20121004

• Small-molecule inhibition of BRDT for male contraception.

  Cell 20120817

• Cancer research: Open ambition.

  Nature 20120809

• Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.

  Bioorganic & medicinal chemistry 20120315

• Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

  Journal of medicinal chemistry 20120126

• Targeting MYC dependence in cancer by inhibiting BET bromodomains.

  Proceedings of the National Academy of Sciences of the United States of America 20111004

• BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

  Cell 20110916

• RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.

  Nature 20110803

• Selective inhibition of BET bromodomains.

  Nature 20101223