Beta-Lapachone

Catalog No.S7261 Synonyms: β-Lapachone, ARQ-501

Beta-Lapachone Chemical Structure

Molecular Weight(MW): 242.27

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
Targets
Topo I [1] IDO1 [4]
0.44 μM
In vitro

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]

In vivo 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]

Protocol

Kinase Assay
+ Expand

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.
Cell Research
+ Expand
  • Cell lines: HL-60, PC-3, DU145, and LNCaP cells
  • Concentrations: 0.005 to 50 μM
  • Incubation Time: 12 hours
  • Method: 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)
Animal Research
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  • Animal Models: Human ovarian cancer cells (36M2) are established in nude mice.
  • Formulation: Lipiodol
  • Dosages: 25–50 mg/kg
  • Administration: Intraperitoneal administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL (136.21 mM) warming
Ethanol 10 mg/mL (41.27 mM)
Water <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 242.27
Formula

C15H14O3

CAS No. 4707-32-8
Storage powder
in solvent
Synonyms β-Lapachone, ARQ-501

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00524524 Completed Advanced Solid Tumors ArQule August 2007 Phase 1
NCT00622063 Completed Cancer ArQule December 2006 Phase 1|Phase 2
NCT00358930 Completed Head and Neck Neoplasms|Carcinoma, Squamous Cell ArQule July 2006 Phase 2
NCT00310518 Completed Cancer ArQule February 2006 Phase 2
NCT00102700 Completed Pancreatic Cancer|Adenocarcinoma ArQule January 2005 Phase 2
NCT00099190 Completed Carcinoma ArQule December 2004 Phase 1

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID