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. 2023 Oct 30;66(21):14787–14814. doi: 10.1021/acs.jmedchem.3c01385

Table 2. Dual Sirt2/HDAC6 Inhibitors Tested by Means of a Biochemical in Vitro Demyristoylation Assay.47a.

compd Sirt2 (demyristoylation)
21 nib
22 nib
31 29 ± 1
32 1.7 ± 0.2
33 9.7 ± 1.3
44 34 ± 2
45 2.8 ± 0.6
46 13.2 ± 1.9
4 1.4 ± 0.3
5 2.5 ± 0.2c
55 nib
56 nib
57 <15% @ 5 μM
SAHA 18% @ 10 μM
a

IC50 values [μΜ, mean ± SD] or percentual inhibition at a given concentration of the dual Sirt2/HDAC6 inhibitors, as well as reference compounds for selective Sirt2 inhibition (4,5), HDAC6 inhibition (5557), and SAHA as an nonselective inhibitor of Zn2+-dependent HDACs.

b

ni = no inhibition (inhibition <15% @ 20 μM).

c

Values for 5 taken from Vogelmann et al.47