β-Lapachone

β-Lapachone is a natural quinone with diverse anti-cancer and anti-inflammatory effects. It inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM).^1,2 In cancer cells which overexpress NAD(P)H:quinone oxidoreductase, β-lapachone is reduced to β-lapachone hydroquinone, which generates reactive oxygen species during its reversion to β-lapachone.³ This process sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.^3,4,5

WARNING This product is not for human or veterinary use.

1. Li, C.J., Averboukh, L., and Pardee, A.B. β-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin. The Journal of Biological Chemisty 268(30), 22463-22468 (1993).

2. Lai, T.-S., Liu, Y., Tucker, T., et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem. Biol. 15(9), 969-978 (2008).

3. Siegel, D., Yan, C., and Ross, D. NAD(P)H:quinone oxidoreductase 1 (NQO1) in the sensitivity and resistance to antitumor quinones. Biochem. Pharmacol. 83(8), 1033-1040 (2012).

4. Dong, G.Z., Oh, E.T., Lee, H., et al. β-Lapachone suppresses radiation-induced activation of nuclear factor-κB. Exp. Mol. Med. 42(5), 327-334 (2010).

5. Li, L.S., Bey, E.A., Dong, Y., et al. Modulating endogenous NQO1 levels identifies key regulatory mechanisms of action of β-lapachone for pancreatic cancer therapy. Clin. Cancer Res. 17, 275-285 (2011).