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化合物(+)-JQ-1,(+)-JQ-1

化合物(+)-JQ-1|T2110主打

價(jià)格 ￥253 ￥357 ￥588
包裝 1mg 2mg 5mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-02
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產(chǎn)品詳情

中文名稱:化合物(+)-JQ-1英文名稱:(+)-JQ-1
CAS:1268524-70-4品牌: TargetMol
產(chǎn)地: 美國(guó)保存條件: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格: ≥95%產(chǎn)品類別: 抑制劑
貨號(hào): T2110
2024-12-02 化合物(+)-JQ-1 (+)-JQ-1 1mg/253RMB;2mg/357RMB;5mg/588RMB 253 TargetMol 美國(guó) keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. ≥95% 抑制劑

Product Introduction

Bioactivity

名稱(+)-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.
細(xì)胞實(shí)驗(yàn)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].
動(dòng)物實(shí)驗(yàn)(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].
體外活性方法：BRD4-NUT 依賴性細(xì)胞系 NMC 797 用 (+)-JQ-1 (250 nM) 處理 48 h，使用 Flow Cytometry 檢測(cè)細(xì)胞周期情況。 結(jié)果：(+)-JQ-1 誘導(dǎo) G1 細(xì)胞周期停滯。[1] 方法：人多發(fā)性骨髓瘤細(xì)胞 KMS11、LR5、OPM1 和 INA-6 用 (+)-JQ-1 (500 nM) 處理 24 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。 結(jié)果：(+)-JQ-1 抑制擴(kuò)增的 Myc 依賴性 MM 細(xì)胞系中對(duì) c-Myc 蛋白表達(dá)。[2]
體內(nèi)活性方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 (+)-JQ-1 (50 mg/kg，5% DMSO in 5% dextrose) 腹腔注射給攜帶 NMC 異種移植瘤的 NCr nude 小鼠，每天一次，持續(xù)十八天。 結(jié)果：(+)-JQ-1 治療后，觀察到明顯的腫瘤消退和總生存率的提高。[1] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 (+)-JQ-1 (50 mg/kg) 腹腔注射給攜帶人胃癌腫瘤 HGC27 的 nude 小鼠，每天一次，持續(xù)兩周。 結(jié)果：(+)-JQ-1 阻止胃癌腫瘤生長(zhǎng)并抑制腫瘤轉(zhuǎn)移。[3]
存儲(chǔ)條件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.
關(guān)鍵字JQ 1 | Inhibitor | (+)JQ1 | JQ-1 | (+) JQ 1 | Autophagy | Epigenetic Reader Domain | inhibit | Target Protein-binding Moiety | Ligands for Target Protein for PROTAC
相關(guān)產(chǎn)品Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate
相關(guān)庫(kù)經(jīng)典已知活性庫(kù) | 抗癌活性化合物庫(kù) | 已知活性化合物庫(kù) | 高選擇性抑制劑庫(kù) | 抗衰老化合物庫(kù) | 抗COVID-19化合物庫(kù)
關(guān)鍵字： JQ1|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。 從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。 經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期 2013-04-18 （12年） 注冊(cè)資本 566.2651萬(wàn)人民幣
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主營(yíng)行業(yè) 化學(xué)試劑,生物活性小分子 經(jīng)營(yíng)模式 貿(mào)易,試劑,定制,服務(wù)
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  • 公司成立：12年
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  • 主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
  • 公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓
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