(+)-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。(+)-JQ-1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
化学信息：
分子量：456.99
分子式： C23H25ClN4O2S
CAS No.： 1268524-70-4
Smiles： CC=1C2=C(N3C([C@H](CC(OC(C)(C)C)=O)N=C2C4=CC=C(Cl)C=C4)=NN=C3C)SC1C
密度： 1.33 g/cm3
储存&溶解度：
存储 keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息：
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.94 mg/mL (6.43 mM), In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol: 45.7 mg/mL (100 mM), Sonication is recommended.
DMSO: 45 mg/mL (98.47 mM), Sonication is recommended.
溶液配制表
DMSO/Ethanol
1mg 5mg 10mg 50mg
10 mM 0.2188 mL 1.0941 mL 2.1882 mL 10.9412 mL
20 mM 0.1094 mL 0.5471 mL 1.0941 mL 5.4706 mL
50 mM 0.0438 mL 0.2188 mL 0.4376 mL 2.1882 mL
Ethanol
1mg 5mg 10mg 50mg
100 mM 0.0219 mL 0.1094 mL 0.2188 mL 1.0941 mL
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