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

Table 1. Dual Sirt2/HDAC6 Inhibitors Tested by Means of Previously Reported Biochemical in Vitro Deacetylation Assays4446a.

compd Sirt2 HDAC6 Sirt1 Sirt3 HDAC1 HDAC2 HDAC3
21 11.5 ± 0.04 0.15 ± 0.01 nib nib 2.1 ± 0.2 nte nte
22 15% @ 10 μM 0.011 ± 0.001 nib nib 0.21 ± 0.03 nte nte
31 0.56 ± 0.27 0.025 ± 0.001 nib nib 0.62 ± 0.06 nte nte
32 0.15 ± 0.01 0.042 ± 0.007 nib 17% @ 20 μM 1.2 ± 0.2 1.8 ± 0.1 0.71 ± 0.03
33 0.32 ± 0.11 0.043 ± 0.003 nib nib 2.2 ± 0.2 6.0 ± 0.2 2.5 ± 0.2
44 0.48 ± 0.04 0.0096 ± 0.0003 nib nib 0.60 ± 0.03 nte nte
45 0.54 ± 0.01 0.017 ± 0.001 nib nib 0.46 ± 0.05 nte nte
46 0.48 ± 0.07 0.0050 ± 0.0005 nib nib 0.21 ± 0.03 0.34 ± 0.02 0.14 ± 0.01
4 0.22 ± 0.01 18% @ 10 μM nib nib 10% @ 10 μM nte nte
5 0.12 ± 0.01c nic,d nic,d nic,d nic,d nte nte
55 nte 0.65 ± 0.04 nte nte 17 ± 1 nte nte
56 nte 0.018 ± 0.001 nte nte 0.81 ± 0.05 nte nte
57 nie 0.032 ± 0.004 nib nib 3.2 ± 0.2 4.7 ± 0.1 4.8 ± 0.4
SAHA nte 0.030 ± 0.008 nte nte 0.12 ± 0.01 0.16 ± 0.01 0.11 ± 0.01
a

IC50 values [μM, 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

d

ni = no inhibition (IC50 > 100 μM).

e

nt = not tested.