Table 2 Most relevant HATi
Compound Structure
Enzyme
inhibitory
activity
Cell-based activity
Ref.
1 Lys-CoA
H 2 N
O
HN
N
H
O
O
SCoA
p300
IC 50 ¼ 0.5 μM
PCAF
IC 50 ¼ 200 μM
–
[72]
5a
Anacardic
acid
OH
O
OH
14
p300/CBP
IC 50 ¼ 5–
1,000 μM
PCAF
IC 50 ¼ 5–
667 μM
Tip60
IC 50 ¼ 64–
348 μM
MOF
IC 50 ¼ 43–
64 μM
Inhibition of p65 subunit
acetylation and subsequent repression of
NF-κB signalling
[74, 77–
79]
9a LoCAM
(SPV106)
OEt
O
EtO
O
13
p300/CBP
74% inhibition
@50 μM
PCAF 137%
activation
@100 μM
Apoptotic and
antiproliferative effects
in human leukaemia
U937 cells
[85, 86]
10
Curcumin
OH O
OH
HO
MeO
OMe
p300
IC 50 ¼ 25 μM
Reduction of p300dependent acetylation of
histone H3/H4 and p53.
Under examination in
many clinical trials for
various indications
[87–91]
11a
Garcinol
O
O
OH O
OH
OH
p300
IC 50 ¼ 7 μM
PCAF
IC 50 ¼ 5 μM
Inhibition of histone
acetylation and induction
of apoptosis in several
cancer cell lines
[93]
11d
EML425
N
N
O
O
O
OH
p300
IC 50 ¼ 2.9 μM
CBP
IC 50 ¼ 1.1 μM
Reduction of H4K5 and
H3K9 acetylation levels
and induction of cell
cycle arrest in the G0/G1
phase (U937 cells)
[96]
12a
NK13650A
O
N
H
HO
O
HO O
COOH
O
NH
HN
N
H
NH2
NH
O
O
HO
R
R ¼ NH-aspartic acid
p300
IC 50 ¼ 11 nM
Repression of transcription mediated by androgen and oestrogen
receptors and
antiproliferative effects
in various cancer cell
lines
[97]
(continued)
104
D. Trisciuoglio and D. Rotili