GN25

The tumor suppressor gene, p53, is often mutated or suppressed in human cancers. Oncogenic K-Ras has been shown to inhibit p53 function by inducing Snail to bind and eliminate p53 through exocytosis. GN25 is a 2-thio-dimethoxy naphthoquinone analog that blocks Snail binding to p53 and induces p53 expression in cancer cells in a K-Ras dependent manner. At 10 μM, GN25 significantly reduces cell proliferation in K-Ras mutated A549 and HCT116 cell lines but not in wild type MKN-45 cells. In a xenograft mouse model, 10 mg/kg GN25 yields antitumoral effects by notably reducing tumor size and progression.¹

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1. Lee, S.H., Shen, G.N., Jung, Y.S., et al. Antitumor effect of novel small chemical inhibitors of Snail-p53 binding in K-Ras-mutated cancer cells. Oncogene 29(32), 4576-4587 (2010).