化合物(+)-JQ-1|T2110

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

￥253 1mg 起订

￥357 2mg 起订

￥588 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物(+)-JQ-1

英文名称：: (+)-JQ-1

CAS号：: 1268524-70-4

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T2110

Product Introduction

Bioactivity

名称	(+)-JQ-1
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.
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].
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]
存储条件	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	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.94 mg/mL (6.43 mM), Please add co-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) DMSO : 45 mg/mL (98.47 mM), Sonication is recommended.
关键字	JQ 1 \| Inhibitor \| (+)JQ1 \| JQ-1 \| (+) JQ 1 \| Autophagy \| Epigenetic Reader Domain \| inhibit \| Target Protein-binding Moiety \| Ligands for Target Protein for PROTAC
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相关库	经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| 抗COVID-19化合物库

JQ1|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子