10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 5 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy
In vitro
(+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. (+)-JQ1 (1 μM) activates HIV transcription in latently infected Jurkat T cells. (+)-JQ1 (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. (+)-JQ1 (5 μM) induces Brd4 dissociation enables Tat to recruit SEC to HIV promoter and induce Pol II CTD phosphorylation and viral transcription in J-Lat A2 cells. JQ1 enables Tat to increase CDK9 T-loop phosphorylation and partially dissociates P-TEFb from 7SK snRNP in Jurkat T cells.
In vivo
(+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts.
Cell Data
cell lines：
Concentrations：~500 nM
Incubation Time：48 hours
Powder Purity:≥99%
| Isomeric SMILES | CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C |
|---|---|
| Molecular Weight | 456.99 |
| Reaxy-Rn | 21994149 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21994149&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Solubility | Solubility (25°C) In vitro DMSO: 103 mg/mL (200.43 mM); Ethanol: 22 mg/mL (42.81 mM); Water: Insoluble; |
|---|---|
| Molecular Weight | 457.000 g/mol |
| XLogP3 | 4.900 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Exact Mass | 456.139 Da |
| Monoisotopic Mass | 456.139 Da |
| Topological Polar Surface Area | 97.600 Ų |
| Heavy Atom Count | 31 |
| Formal Charge | 0 |
| Complexity | 706.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
| 1. Lujing Geng, Tong Lu, Huaqing Jing, Yue Zhou, Xiaoyang Liang, Jiao Li, Nan Li. (2022) Iron-based and BRD4-downregulated strategy for amplified ferroptosis based on pH-sensitive/NIR-II-boosted nano-matchbox. Acta Pharmaceutica Sinica B, [PMID:36873167] [10.1016/j.apsb.2022.05.011] |
| 2. Xiao-Kang Jin, Jun-Long Liang, Shi-Man Zhang, Qian-Xiao Huang, Shun-Kang Zhang, Chuan-Jun Liu, Xian-Zheng Zhang. (2023) Orchestrated copper-based nanoreactor for remodeling tumor microenvironment to amplify cuproptosis-mediated anti-tumor immunity in colorectal cancer. Materials Today, [PMID:] [10.1016/j.mattod.2023.06.024] |
| 3. Maoyu Gao, Kai Feng, Xinmiao Zhang, Yiling Ruan, Guizhen Zhao, Huihui Liu, Xiaolian Sun. (2023) Nanoassembly with self-regulated magnetic thermal therapy and controlled immuno-modulating agent release for improved immune response. JOURNAL OF CONTROLLED RELEASE, [PMID:36948418] [10.1016/j.jconrel.2023.03.035] |
| 4. Xinpei Wang, Xu Chen, Zhidong Chen, Wanting Xu, Ruizhi Lai, Xiaohui Qiu, Zekai Zeng, Chenglin Wang, Zhe Wang, Junqing Wang. (2024) Integrated Anchored Stapling and Hierarchical Dynamics: MSICDA-Driven CREBBP Bromodomain Inhibition. Journal of Chemical Information and Modeling, [PMID:38863138] [10.1021/acs.jcim.4c00381] |
| 5. Lingling Wei, Haoyu Jin, Zhongke Ji, Haoyang Tian, Jiayang Han, Yanyan Liu, Wanjia Li, Di Liu, Hui Song. (2026) Amplifying the “In Situ Vaccination” of BET Inhibition via Autophagy Blockade: Mechanism and Local Delivery in OSCC. Journal of Materials Chemistry B, [PMID:41631619] [10.1039/D5TB02525G] |
