(+)-JQ1

製品コードS7110 バッチS711015

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H25ClN4O2S
分子量 456.99 CAS No. 1268524-70-4
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 91 mg/mL (199.12 mM)
Ethanol 91 mg/mL (199.12 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2% DMSO 30% PEG 300 5%Tween80 63%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 3.340mg/ml (7.31mM) Taking the 1 mL working solution as an example, add 20 μL of 167 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 630 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.500mg/ml (9.85mM) Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

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.
in vitro (+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. This compound (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. This chemical (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. This compound (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. It inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. [1] It results in robust inhibition of MYC expression in MM cell lines. This compound inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. This chemical (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. It (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. This compound (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. [2] It inhibits growth of LP-1 cells with GI50 of 98 nM. This chemical (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. It (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. [3] This compound (1 μM) activates HIV transcription in latently infected Jurkat T cells. It (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. This chemical (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. It 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. This compound results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. It induces strong (grade 31) keratin expression in NMC 797 xenografts. This chemical promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. [1] It 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] This compound 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
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).
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

  • https://pubmed.ncbi.nlm.nih.gov/20871596/
  • https://pubmed.ncbi.nlm.nih.gov/21889194/
  • https://pubmed.ncbi.nlm.nih.gov/21949397/
  • https://pubmed.ncbi.nlm.nih.gov/23087374/

カスタマーフィードバック

Data from [Cancer Res, 2014, 74(23), 7090-102]

Data from [Cancer Res, 2014, 74(23), 7090-102]

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：

MYC ecDNA promotes intratumour heterogeneity and plasticity in PDAC [ Nature, 2025, 10.1038/s41586-025-08721-9] PubMed: 40074906
The ESCRT protein CHMP5 promotes T cell leukemia by enabling BRD4-p300-dependent transcription [ Nat Commun, 2025, 16(1):4133] PubMed: 40319015
Super-enhancer-driven EFNA1 fuels tumor progression in cervical cancer via the FOSL2-Src/AKT/STAT3 axis [ J Clin Invest, 2025, e177599] PubMed: 39964764
BACH2 promotes seeding and establishment of long-lived HIV-1 reservoir in memory CD4+ T cells [ Cell Rep Med, 2025, S2666-3791(25)00384-2] PubMed: 40845840
Elevated Transglutaminase-2 in SOX10-Deficient Melanoma Promotes Tumor Onset and Decreases Intratumoral CD4+ T Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-3267] PubMed: 40742313
(+)-JQ-1 alleviates cardiac injury in myocardial infarction by inhibiting ferroptosis through the NAMPT/SIRT1 pathway [ Cell Death Dis, 2025, 16(1):548] PubMed: 40695797
GDP-mannose 4,6-dehydratase is a key driver of MYCN-amplified neuroblastoma core fucosylation and tumorigenesis [ Oncogene, 2025, 10.1038/s41388-025-03297-0] PubMed: 39956863
Androgen-induced AR-BRD4 transcriptional regulatory complex promotes malignant proliferation of osteosarcoma cells [ Cell Death Discov, 2025, 11(1):272] PubMed: 40494882
USP35 promotes the growth of ER positive breast cancer by inhibiting ferroptosis via BRD4-SLC7A11 axis [ Commun Biol, 2025, 8(1):64] PubMed: 39820080
Leveraging automated time-lapse microscopy coupled with deep learning to automate colony forming assay [ Front Oncol, 2025, 15:1520972] PubMed: 40046624

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。