The tumor suppressor function of p53 hinges on its ability to function as a transcription factor. Tenovin-6 is an analog of tenovin-1, a small molecule activator of p53 transcriptional activity. At 10 μM, this compound is slightly more effective than tenovin-1 at elevating p53 activity in MCF-7 cells and reduces growth of ARN8 melanoma xenograft tumors in SCID mice at a dose of 50 mg/kg. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 μM, respectively.
