Background
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 ?M, 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.1 Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 ?M, respectively.1
1.Lain, S., Hollick, J.J., Campbell, J., et al.Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activatorCancer Cell13(5)454-463(2008)
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