化合物Beta-Lapachone|T6407

β-Lapachone
4707-32-8

￥148 1mg 起订

￥297 5mg 起订

￥493 10mg 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Beta-Lapachone

英文名称：: β-Lapachone

CAS号：: 4707-32-8

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.81%

产品类别：: 抑制剂

货号：: T6407

Product Introduction

Bioactivity

名称	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.
细胞实验	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)
激酶实验	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.
体外活性	Beta-Lapachone通过剂量依赖性方式抑制由DNA拓扑异构酶I引起的DNA松弛。[1] 对Beta-Lapachone（100 nM或更高浓度）的处理导致与DMSO对照相比，Topo I DNA解旋活性的抑制率超过95%。Beta-Lapachone（1-5 μM）通过锁定Topo I到DNA上并阻止复制叉移动，导致HL-60和三种人类前列腺癌细胞（DU-145, PC-3, 和LNCaP）的细胞周期在G0/G1阶段停滞并诱导细胞凋亡。[2] Beta-Lapachone促进小鼠3T3成纤维细胞和人类内皮EAhy926细胞通过不同的MAPK信号途径迁移，从而在体外加速刮擦伤口的愈合。[3] 此外，Beta-Lapachone通过不竞争性抑制作用抑制纯化的重组IDO1活性，IC50为0.44 μM；且Beta-Lapachone还展示出具有IC50为1.0 μM的高效细胞内IDO1抑制活性，该活性部分依赖于NQO1的生物转化。[4] Beta-Lapachone通过NQO1依赖性的活性氧（ROS）生成和PARP1过度激活诱导NQO1+癌细胞的程序性坏死。[5]
体内活性	Beta-lapachone (50 mg/kg) 的处理在人类卵巢癌异种移植小鼠模型中显著抑制体内肿瘤生长，且与taxol联合使用可协同诱导凋亡。[6] 在正常及糖尿病(db/db)小鼠中，beta-lapachone的治疗相比于仅用载体的治疗可加速愈合过程。[3]
存储条件	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)
关键字	NSC26326 \| Topoisomerase \| b-Lapachone \| Inhibitor \| β-Lapachone \| NSC 26326 \| Apoptosis \| ARQ501 \| ARQ 501 \| Autophagy \| β Lapachone \| inhibit \| βLapachone \| SL 11001 \| SL11001
相关产品	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
相关库	抑制剂库 \| 经典已知活性库 \| 植物来源化合物库 \| 已知活性化合物库 \| 抗癌天然产物库 \| 抗衰老化合物库 \| 天然产物库 \| 中药单体化合物库 \| 药物功能重定位化合物库 \| 高通量筛选天然产物库

SL-11001|||NSC-26326|||Beta-Lapachone|||ARQ-501|||3,4-二氢-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮|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