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受注：045-509-1970 |
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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C23H25ClN4O2S |
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| 分子量 | 456.99 | CAS No. | 1268524-70-4 | |
| Solubility (25°C)* | 体外 | DMSO | 91 mg/mL warmed with 50ºC water bath (199.12 mM) | |
| Ethanol | 91 mg/mL (199.12 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | (+)-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. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| 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. [1] (+)-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. [2] (+)-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. [3] (+)-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. [4] |
| 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. [1] (+)-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. [2] (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. [3] |
| 特徴 | (+)-JQ1 is more effective than (-)-JQ1. |
プロトコル(参考用のみ)
| 細胞アッセイ | 細胞株 | MC 11060 cells |
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| 濃度 | ~500 nM | |
| 反応時間 | 48 hours | |
| 実験の流れ | Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism). |
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| 動物実験 | 動物モデル | Mice bearing NMC 797 xenografts |
| 投薬量 | 50 mg/kg | |
| 投与方法 | intraperitoneal injection |
参考
カスタマーフィードバック
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Data from [Cancer Res, 2014, 74(23), 7090-102]
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Data from [Cancer Res, 2014, 74(23), 7090-102]
-JQ1-S711001Y0120170215.gif)
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Data from [Data independently produced by , , Sci Rep, 2016, 6:23770.]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
| Inhibition of spinal BRD4 alleviates pyroptosis and M1 microglia polarization via STING-IRF3 pathway in morphine-tolerant rats [ Eur J Pharmacol, 2024, 969:176428] | PubMed: 38432572 |
| The ESCRT protein CHMP5 promotes T cell leukemia by controlling BRD4-p300-dependent transcription [ bioRxiv, 2024, 2024.01.29.577409] | PubMed: 38352301 |
| NSD2 is a requisite subunit of the AR/FOXA1 neo-enhanceosome in promoting prostate tumorigenesis [ bioRxiv, 2024, 2024.02.22.581560] | PubMed: 38464251 |
| BRD4-targeting PROTAC as a unique tool to study biomolecular condensates [ Cell Discov, 2023, 9(1):47] | PubMed: 37156794 |
| Senescence Rewires Microenvironment Sensing to Facilitate Antitumor Immunity [ Cancer Discov, 2023, 13(2):432-453] | PubMed: 36302222 |
| Senescence Rewires Microenvironment Sensing to Facilitate Antitumor Immunity [ Cancer Discov, 2023, 13(2):432-453] | PubMed: 36302222 |
| Defining the landscape of circular RNAs in neuroblastoma unveils a global suppressive function of MYCN [ Nat Commun, 2023, 14(1):3936] | PubMed: 37402719 |
| Context-dependent perturbations in chromatin folding and the transcriptome by cohesin and related factors [ Nat Commun, 2023, 14(1):5647] | PubMed: 37726281 |
| Context-dependent perturbations in chromatin folding and the transcriptome by cohesin and related factors [ Nat Commun, 2023, 14(1):5647] | PubMed: 37726281 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。