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IL06501 β-兰帕科恩(10mM in DMSO,无菌

) 抑制剂/拮抗剂/激动剂 索莱宝
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  • ¥970
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  • 北京
  • IL06501
  • 2025年07月23日
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    • 详细信息
    • 技术资料
    • 保存条件

      Stroe at -20℃,6 months.

    • 保质期

      Stroe at -20℃,6 months.

    • 英文名

      beta-Lapachone(10mM in DMSO,Sterile)

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      4707-32-8

    • 规格

      1ml

    基本信息
    CASNo.4707-32-8
    中文名称β-兰帕科恩(10mM in DMSO,无菌)
    英文名称beta-Lapachone(10mM in DMSO,Sterile)
    分子式C15H14O3
    分子量242.27
    溶解性请根据自己的实验要求使用。
    外观(性状)无菌溶液
    储存条件Stroe at -20℃,6 months.
    靶点Topoisomerase
    通路DNA Damage/DNA Repair
    背景说明β-Lapachone 是一种萘醌类化合物,是拓扑异构酶 I (topoisomerase I) 抑制剂。
    生物活性β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.[1-3]
    In Vitroβ-Lapachone is a topoisomerase I inhibitor. β-Lapachone (25 μM) inhibits camptothecin-induced DNA cleavage[1]. β-Lapachone (10-40 μM) significantly reduces the colony-forming ability of CHO cells, and is cytotoxic in S phase. β-Lapachone at above 10 μM, causes a heavy DNA-strand breaks in CHO cells[2]. β-Lapachone (10 μM) suppresses JCPyV replication in IMR-32 cells. β-Lapachone (1.0?μM) potently affects JCPyV propagation in JCI cells. β-Lapachone (0.01-0.1 μM) inhibits VP1 production in JCI cells[4].
    细胞实验β-Lapachone (0.066%) ameliorates cisplatin-induced renal injury and when in combination with cisplatin, the affect is more significant in mice. β-Lapachone increases Mre11-Rad50-Nbs1 (MRN) complex expression in mice[3].
    细胞实验Cytotoxicity is measured by an MTT assay. IMR-32 and JCI cells are plated in 96-well microtiter plates at a concentration of 5.0?×?104 (topotecan) or 2.5?×?104 (β-lapachone) cells/well/100?μL medium 24 hr prior to addition of various concentrations of topotecan or β-lapachone. The cells are then incubated for 72?hr at 37°C in a CO2 incubator. Cell proliferation is assessed using a Cell Proliferation Kit I. Experiments are performed using four independent cultures[4].
    动物实验Male Balb/c mice are provided a commercial pellet diet and water ad libitum. After 1 week of acclimation, the mice are randomly allocated to one of the following groups (5 per group): control, β-lapachone, cisplatin (18 mg/kg, ip), and β-lapachone + cisplatin (18 mg/kg, ip). The β-lapachone groups are fed a diet containing the drug (0.066) for 2 weeks prior to cisplatin injection. All mice are sacrificed under carbon dioxide anesthesia 3 days after cisplatin injection. The blood samples are subjected to serum BUN and CRE analyses. Half of the kidney is quickly removed for histopathological and immunohistochemical (IHC) studies. The other half is stored at ?70°C until western blot assay[3].
    激酶实验DNA topoisomerase I is incubated in the presence or absence of drugs (including β-Lapachone), in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCl, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 min at 37°C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-h 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[1].
    数据来源文献[1]. Li CJ, et al. beta-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin. J Biol Chem. 1993 Oct 25;268(30):22463-8.
    [2]. Vanni A, et al. DNA damage and cytotoxicity induced by beta-lapachone: relation to poly(ADP-ribose) polymerase inhibition. Mutat Res. 1998 Jun 5;401(1-2):55-63.
    [3]. Kim TW, et al. β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity. Pharmacol Rep. 2016 Feb;68(1):27-31.
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