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(+)-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。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

(+)-JQ-1, CAS 1268524-70-4

规格	价格/CNY	货期
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

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其他形式的 (+)-JQ-1:

(R)-(-)-JQ1 Enantiomer
现货
JQ-1 (carboxylic acid)
现货

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%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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), Sonication 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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

=

浓度

X

容积

X

分子量

浓度 (起始)

X

容积 (起始)

=

浓度 (终)

X

容积 (终)

溶液体积

=

质量

/

配液浓度

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.

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

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

g

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

%

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

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

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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(+)-JQ-1

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords