Norcantharidin

Norcantharidin is a demethylated form of the protein phosphatase 1 (PP1) and PP2A inhibitor cantharidin (Item No. 14589) and a PP1 and PP2A inhibitor (IC₅₀s = 9 and 3 µM, respectively).^1,2 It induces cell cycle arrest at the G₂/M phase and apoptosis in HepG2, Hep3B, and Huh7 human hepatoma cell lines when used at a concentration of 5 µg/ml.² Norcantharidin (500-5,000 µg/ml) reduces angiogenesis in a chick chorioallantoic membrane assay.³ It inhibits growth in a panel of nine human cancer cell lines, including breast, lung, skin, and glioblastoma cancer cells, with GI₅₀ values ranging from 30 to 64 µM.¹ Norcantharidin (28 mg/kg, i.p.) reduces tumor growth in a GBC-SD mouse xenograft model.

WARNING This product is not for human or veterinary use.

1. Hill, T.A., Stewart, S.G., Sauer, B., et al. Heterocyclic substituted cantharidin and norcantharidin analogues - synthesis, protein phosphatase (1 and 2A) inhibition, and anti-cancer activity. Bioorg. Med. Chem. Lett. 17(12), 3392-3397 (2007).

2. Chen, Y.-N., Chen, J.-C., Yin, S.-C., et al. Effector mechanisms of norcantharidin-induced mitotic arrest and apoptosis in human hepatoma cells. Int. J. Cancer 100(2), 158-165 (2002).

3. Zhang, J.-T., Fan, Y.-Z., Chen, C.-Q., et al. Norcantharidin: A potential antiangiogenic agent for gallbladder cancers in vitro and in vivo. Int. J. Oncol. 40(5), 1501-1514 (2012).