FIGURE 1. Identification of potent SIRT1 activators unrelated to resveratrol.
From the following article:
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes
Jill C. Milne, Philip D. Lambert, Simon Schenk, David P. Carney, Jesse J. Smith, David J. Gagne, Lei Jin, Olivier Boss, Robert B. Perni, Chi B. Vu, Jean E. Bemis, Roger Xie, Jeremy S. Disch, Pui Yee Ng, Joseph J. Nunes, Amy V. Lynch, Hongying Yang, Heidi Galonek, Kristine Israelian, Wendy Choy, Andre Iffland, Siva Lavu, Oliver Medvedik, David A. Sinclair, Jerrold M. Olefsky, Michael R. Jirousek, Peter J. Elliott & Christoph H. Westphal
Nature 450, 712-716(29 November 2007)
doi:10.1038/nature06261

a, Chemical structures of SIRT1 activators, resveratrol, SRT1460, SRT2183, and SRT1720. b, The effect of activators on human SIRT1 enzyme activity measured by mass spectrometry. c, Cellular activity was measured using an ICW that monitors the degree of p53 deacetylation in U2OS cells using
-tubulin as a normalization control. Compounds were tested at concentrations of: resveratrol (100
M), SRT2183 (10
M), SRT1460 (10
M), SRT1720 (0.10
M). Each concentration represents the approximate EC50 for each compound. n = 6 for all compounds tested except for resveratrol, where n = 3. Data are expressed as mean
s.d. The activation of SIRT1 resulting in p53 deacetylation could be blocked by a SIRT1 inhibitor, 6-chloro-2,3,4,9-tetrahydro-1-H-carbazole-1-carboxamide (10
M). n = 3 for all compounds tested.
