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β-Lapachone

β-Lapachone (ARQ-501) 是一种萘醌类天然产物，是拓扑异构酶 I 抑制剂，通过抑制细胞周期进程来诱导细胞凋亡。

CAS号

4707-32-8

分子式

C15H14O3

主要靶点

Apoptosis|Autophagy|IDO|Topoisomerase

仅限科研使用

Cat No : CM00593

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Synonyms

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

验证数据展示

  • CAS No.: 4707-32-8

    β-Lapachone
    CAS#: 4707-32-8

产品信息

β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.

CAS号 4707-32-8
分子式 C15H14O3
主要靶点 Apoptosis|Autophagy|IDO|Topoisomerase
主要通路 凋亡|自噬|DNA损伤和修复|代谢
分子量 242.27
纯度 99.64%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 3,4-二氢-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮|SL-11001|NSC-26326|Beta-Lapachone|ARQ-501

靶点活性

IDO1:0.44 μM

体内活性

Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. [6] In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only. [3]

体外活性

Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. [1] Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. [2] Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. [3] In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. [4] Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. [5]

溶解度

Ethanol:12.1 mg/mL (50 mM),DMSO:24.2 mg/mL (100 mM)

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)

参考文献

1.Li CJ, et al. J Biol Chem. 1993, 268(30), 22463-22468.
2.Planchon SM, et al. Cancer Res. 1995, 55(17), 3706-3711.
3.Kung HN, et al. Am J Physiol Cell Physiol. 2008, 295(4), C931-943.
4.Flick HE, et al. Int J Tryptophan Res. 2013, 6, 35-45.
5.Huang X, et al. Cancer Res. 2012, 72(12), 3038-3047.
6.Kim TW, et al. β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity. Pharmacol Rep. 2016 Feb;68(1):27-31.
7.Wu L, Ma X, Yang X, et al. Synthesis and biological evaluation of β-lapachone-monastrol hybrids as potential anticancer agents[J]. European Journal of Medicinal Chemistry. 2020: 112594.

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