So far, several SIRT1 and SIRT2 inhibitors have been developed (Fig. 1), including e.g. salermide (1),27 AC93253 (2),28 tenovin-6 (3),29,30 TM (4),31 SirReal2 (5),32,33 3′-phenethyloxy-2-anilinobenzamide (6),34 AGK2 (7),35 AK-1 (8)36 and EX-527 (9).37 These compounds have shown antiproliferative activity when tested in cancer cells and some of these have shown beneficial effects in neurological disorder models, but in many cases, the lack of potency and isoform specificity suggests their effect is not solely related to SIRT1/2 inhibition. Here, SIRT1 is linked to cancer.