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. Author manuscript; available in PMC: 2015 Apr 3.
Published in final edited form as: Future Med Chem. 2014 May;6(8):945–966. doi: 10.4155/fmc.14.44

Table 6.

Sirtuin inhibitors: Indole derivatives

Entry # Structure IC50 Biology Activity
1 EX527
graphic file with name nihms674398t35.jpg
SIRT1: 60–100 nM[127] Induced apoptosis in leukemia cell when combined with HDAC inhibitors[135]; protected against OPMD [119]
2 AC-93253
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SIRT1: 45.3 μM
SIRT2: 6 μM
SIRT3: 24.6 μM[48]
Cytotoxic effects in prostate DU145, pancreas MiaPaCa, lung A549 and NCI-H460 cancer cell lines[48]
3 Inauhzin (INZ)
graphic file with name nihms674398t37.jpg
SIRT1: 0.7–2 μM[130] Inhibited cell proliferation, induced senescence and apoptosis of human cancer cell without genotoxicity, and repressed the growth of xenograft tumors derived from human lung cancer H460 and colon cancer HCT116 cells harbouring p53[130].
4 Ro31-8220
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SIRT1: 3.5 μM
SIRT2: 0.8 μM[132]
5 GW5074
graphic file with name nihms674398t39.jpg
SIRT1: 41.6 μM [133]
SIRT2: 15.6 μM [133]
SIRT3: 25.1 μM [133]
SIRT5: 19.5 μM [134]