化合物Beta-Lapachone|T6407

價(jià)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	2024-09-14

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產(chǎn)品詳情

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(hào): T6407

Product Introduction

Bioactivity

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(xì)胞實(shí)驗(yàn)	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(shí)驗(yàn)	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?fù)洚悩?gòu)酶I引起的DNA松弛。[1] 對(duì)Beta-Lapachone（100 nM或更高濃度）的處理導(dǎo)致與DMSO對(duì)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(fù)制叉移動(dòng)，導(dǎo)致HL-60和三種人類前列腺癌細(xì)胞（DU-145, PC-3, 和LNCaP）的細(xì)胞周期在G0/G1階段停滯并誘導(dǎo)細(xì)胞凋亡。[2] Beta-Lapachone促進(jìn)小鼠3T3成纖維細(xì)胞和人類內(nèi)皮EAhy926細(xì)胞通過不同的MAPK信號(hào)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(jìng)爭(zhēng)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(xì)胞內(nèi)IDO1抑制活性，該活性部分依賴于NQO1的生物轉(zhuǎn)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(dǎo)NQO1+癌細(xì)胞的程序性壞死。[5]
體內(nèi)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(nèi)腫瘤生長，且與taxol聯(lián)合使用可協(xié)同誘導(dǎo)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(chǔ)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(guān)鍵字	NSC26326 \| Topoisomerase \| b-Lapachone \| Inhibitor \| β-Lapachone \| NSC 26326 \| Apoptosis \| ARQ501 \| ARQ 501 \| Autophagy \| β Lapachone \| inhibit \| βLapachone \| SL 11001 \| SL11001
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相關(guān)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

關(guān)鍵字： 3,4-二氫-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮|||Beta-Lapachone|||NSC-26326|||SL-11001|||ARQ-501|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，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)過在中國市場(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	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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