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(+)-JQ-1

(+)-JQ-1

产品编号 T2110   CAS 1268524-70-4
别名: JQ1

(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂,抑制 BRD4(1/2) (IC50=77/33 nM),具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬,抑制细胞增殖。

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(+)-JQ-1 Chemical Structure
(+)-JQ-1, CAS 1268524-70-4
规格 价格/CNY 货期 数量
1 mg ¥ 253 现货
2 mg ¥ 357 现货
5 mg ¥ 588 现货
10 mg ¥ 863 现货
25 mg ¥ 1,360 现货
50 mg ¥ 1,860 现货
100 mg ¥ 2,950 现货
200 mg ¥ 3,580 现货
500 mg ¥ 4,850 现货
1 mL * 10 mM (in DMSO) ¥ 657 现货
其他形式的 (+)-JQ-1:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: (+)-JQ-1 (T2110)
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选择批次  
纯度: 99.97%
纯度: 98.36%
纯度: 98.15%
纯度: 98.00%
纯度: 98%
纯度: 97.57%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 (+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
靶点活性 BRD4(1):77 nM(cell free), BRD4(2):33 nM(cell free)
体外活性 方法:BRD4-NUT 依赖性细胞系 NMC 797 用 (+)-JQ-1 (250 nM) 处理 48 h,使用 Flow Cytometry 检测细胞周期情况。
结果:(+)-JQ-1 诱导 G1 细胞周期停滞。[1]
方法:人多发性骨髓瘤细胞 KMS11、LR5、OPM1 和 INA-6 用 (+)-JQ-1 (500 nM) 处理 24 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:(+)-JQ-1 抑制扩增的 Myc 依赖性 MM 细胞系中对 c-Myc 蛋白表达。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 (+)-JQ-1 (50 mg/kg,5% DMSO in 5% dextrose) 腹腔注射给携带 NMC 异种移植瘤的 NCr nude 小鼠,每天一次,持续十八天。
结果:(+)-JQ-1 治疗后,观察到明显的肿瘤消退和总生存率的提高。[1]
方法:为检测体内抗肿瘤活性,将 (+)-JQ-1 (50 mg/kg) 腹腔注射给携带人胃癌肿瘤 HGC27 的 nude 小鼠,每天一次,持续两周。
结果:(+)-JQ-1 阻止胃癌肿瘤生长并抑制肿瘤转移。[3]
细胞实验 Cells were plated at 5,000 cells per well of 96-well plates containing titrations of the compounds as indicated. After incubation, the cells were washed once with PBS and resuspended in 175 μL of ice-cold 70% ethanol and fixed for a minimum of 16 h at 4 °C. The cells were pelleted and washed 1× with PBS and stained for 30 min at room temperature (RT) with 120 μL of staining solution [propidium iodide (20 μg/mL), RNase A (25 μg/mL), 0.1% Triton X-100 in PBS]. Cell number and cell cycle data were obtained by using a flow cytometer using the Express Pro module. DNA content histograms were analyzed by using ModFit LT 3.2 Software. To calculate the number of viable cells in each well, the concentration of events measured using the Guava was multiplied by the volume of cells in the well, then by the fraction of cells in G1+S+G2/M. GI50 values for each cell line were calculated as the concentration of compound giving a 50% reduction in cell number relative to the DMSO control [4].
动物实验 (Harlan) inoculated s.c. with 3 × 10^6 cells per mouse resuspended in 10% Matrigel. Two weeks later (average tumor volume 150 mm3), mice were assigned into two groups: 15 mice were treated with vehicle control (5:95 DMSO:10% 2-Hydroxypropyl-β-cyclodextrin), and 15 mice were treated with 30 mg/kg (+)-JQ1 by i.p. injection twice a day for 28 d. Body weight and tumor volume were measured daily. Tumor volume was calculated from caliper measurements by using the following formula: W × H × L × 0.52. Mice were killed when tumor volume reached 2,000 mm3, when body weight decreased >20% of initial weight, or when the mice were in poor health as established in the IACUC protocol. Survival was plotted and analyzed in GraphPad Prism software, and statistical significance was calculated by using log-rank (Mantel-Cox) and Gehan–Breslow–Wilcoxon tests. MV4-11 xenografts were established in nude mice injected with 10 × 10^6 cells per mouse. JQ1 was dosed i.p. and formulated as described above. Mice were divided into 4 groups of 10 animals: vehicle control once a day; 50 mg/kg (+)-JQ1 once a day; 30 mg/kg (+)-JQ1 twice a day; and cytarabine 100 mg/kg daily (5 d on, 2 d off). Treatment of mice with cytarabine at 100 mg/kg resulted in significant weight loss at day 8 and, therefore, the dose needed to be decreased to 75 mg/kg [4].
别名 JQ1
分子量 456.99
分子式 C23H25ClN4O2S
CAS No. 1268524-70-4

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 45.7 mg/mL (100 mM)

DMSO: 29.41 mg/mL (64.36 mM), Sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1882 mL 10.9412 mL 21.8823 mL 54.7058 mL
5 mM 0.4376 mL 2.1882 mL 4.3765 mL 10.9412 mL
10 mM 0.2188 mL 1.0941 mL 2.1882 mL 5.4706 mL
20 mM 0.1094 mL 0.5471 mL 1.0941 mL 2.7353 mL
50 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0941 mL
Ethanol 100 mM 0.0219 mL 0.1094 mL 0.2188 mL 0.5471 mL

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TargetMol Library Books参考文献

1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. 2. Delmore JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell. 2011 Sep 16;146(6):904-17. 3. Zhou S, et al. BET protein inhibitor JQ1 downregulates chromatin accessibility and suppresses metastasis of gastric cancer via inactivating RUNX2/NID1 signaling. Oncogenesis. 2020 Mar 10;9(3):33. 4. Mertz JA, et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74. 5. Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma[J]. International Immunopharmacology. 2019, 76: 105921.

TargetMol Library Books文献引用

1. Ding L, Chen X, Zhang W, et al.Canagliflozin primes antitumor immunity by triggering PD-L1 degradation in endocytic recycling.The Journal of Clinical Investigation.2023, 133(1). 2. Ma J, Hu W, Liu Y, et al.CD226 maintains regulatory T cell phenotype stability and metabolism by the mTOR/Myc pathway under inflammatory conditions.Cell Reports.2023, 42(10). 3. Wu T Y, Chen X C, Tang G X, et al.Development and Characterization of Benzoselenazole Derivatives as Potent and Selective c-MYC Transcription Inhibitors.Journal of Medicinal Chemistry.2023 4. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 5. Ding D, Zheng R, Tian Y, et al. Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer. Nature Communications. 2022, 13(1): 1-15. 6. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 7. Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma. International Immunopharmacology. 2019, 76: 105921
GSK9311 Dbet57 I-BET762 carboxylic acid EML 425 BAZ1A-IN-1 666-15 CPI-0610 carboxylic acid TTK21

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 高选择性抑制剂库 NO PAINS 化合物库 抗COVID-19化合物库 细胞重编程化合物库 临床前化合物库 表观遗传库 PPI抑制剂库 表型筛选靶点鉴定库 组蛋白修饰化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

(+)-JQ-1 1268524-70-4 Autophagy Chromatin/Epigenetic PROTAC Epigenetic Reader Domain Ligands for Target Protein for PROTAC JQ 1 Inhibitor (+)JQ1 JQ-1 (+) JQ 1 inhibit JQ1 Target Protein-binding Moiety inhibitor

 

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