價格 | ¥148 | ¥297 | ¥493 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
中文名稱:化合物Beta-Lapachone | 英文名稱:β-Lapachone |
CAS:4707-32-8 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.81% | 產(chǎn)品類別: 抑制劑 |
貨號: T6407 |
名稱 | β-Lapachone |
描述 | β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase. |
細胞實驗 | IC50 calculations for each cell line are determined by DNA amount (IS) and anchorage-dependent colony formation (CF) assays. For the CF assay, cells are seeded at 500 viable cells/well in 6-well plates and incubated overnight, then treated with equal volumes of media containing beta-lapachone at final concentrations ranging from 0.005 to 50 μM in half-log increments (controls were treated with 0.25% DMSO, equivalent to the highest dose of beta-lapachonc used) for 4 hour or for continuous 12-hour exposures. Plates (3 wells/condition) are stained with crystal violet, and colonies of >50 normal-appearing cells are enumerated. IC50 values for various cells are calculated using drug doses with numbers of colonies surrounding 50% of control. For DNA assays, plates are harvested for IC50 determinations 8 days after treatment using a CytoFluor 2350 fluorescence measurement system. Six-well samplings are included in the calculation of DNA fluor units for each dose. A graph of beta-lapachone dose versus percentage control DNA in fluor units is used to calculate each IC50. All experiments are repeated at least twice, each in duplicate. (Only for Reference) |
激酶實驗 | Topoisomerase I Catalytic Actioity Assay [1]: Topoisomerase I Catalytic Actioity Assay: The enzymatic activity is analyzed by the DNA unwinding assay. DNA topoisomerase I, from TopoGEN (1 unit, which is defined as the amount of enzyme that converts 0.5 μg of superhelical DNA to the relaxed state in 30 minutes at 37 °C), is incubated with 0.5 μg of 6x174 RF DNA, in the presence or absence of Beta-Lapachone, in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCI, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 minutes at 37 °C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-hour incubation at 37 °C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system. |
體外活性 | Beta-Lapachone通過劑量依賴性方式抑制由DNA拓撲異構酶I引起的DNA松弛。[1] 對Beta-Lapachone(100 nM或更高濃度)的處理導致與DMSO對照相比,Topo I DNA解旋活性的抑制率超過95%。Beta-Lapachone(1-5 μM)通過鎖定Topo I到DNA上并阻止復制叉移動,導致HL-60和三種人類前列腺癌細胞(DU-145, PC-3, 和LNCaP)的細胞周期在G0/G1階段停滯并誘導細胞凋亡。[2] Beta-Lapachone促進小鼠3T3成纖維細胞和人類內皮EAhy926細胞通過不同的MAPK信號途徑遷移,從而在體外加速刮擦傷口的愈合。[3] 此外,Beta-Lapachone通過不競爭性抑制作用抑制純化的重組IDO1活性,IC50為0.44 μM;且Beta-Lapachone還展示出具有IC50為1.0 μM的高效細胞內IDO1抑制活性,該活性部分依賴于NQO1的生物轉化。[4] Beta-Lapachone通過NQO1依賴性的活性氧(ROS)生成和PARP1過度激活誘導NQO1+癌細胞的程序性壞死。[5] |
體內活性 | Beta-lapachone (50 mg/kg) 的處理在人類卵巢癌異種移植小鼠模型中顯著抑制體內腫瘤生長,且與taxol聯(lián)合使用可協(xié)同誘導凋亡。[6] 在正常及糖尿病(db/db)小鼠中,beta-lapachone的治療相比于僅用載體的治療可加速愈合過程。[3] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 12.1 mg/mL (50 mM) DMSO : 50 mg/mL (206.38 mM) |
關鍵字 | NSC26326 | Topoisomerase | b-Lapachone | Inhibitor | β-Lapachone | NSC 26326 | Apoptosis | ARQ501 | ARQ 501 | Autophagy | β Lapachone | inhibit | βLapachone | SL 11001 | SL11001 |
相關產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
相關庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 植物來源化合物庫 | 已知活性化合物庫 | 抗癌天然產(chǎn)物庫 | 抗衰老化合物庫 | 天然產(chǎn)物庫 | 中藥單體化合物庫 | 藥物功能重定位化合物庫 | 高通量篩選天然產(chǎn)物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務 |
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