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. 2022 Oct 3;13:960263. doi: 10.3389/fgene.2022.960263

TABLE 2.

Structure of HDACs inhibitors against deacetylase isozymes in lung cancer and clinical assays.

Structure HDAC inhibitors In vitro tests NSCLC cell lines HDAC class HDAC isozyme HDAC Inhibition IC50 (nM) Clinical assays Reference
Panobinostat (LBH-589)Inline graphic A549
Calu-1
H226
H460
H838
SKMES-1
Class I
Class IIa
Class IIb
HDAC-1
HDAC-2
HDAC-3
HDAC-8
HDAC-4
HDAC-7
HDAC-9
HDAC-6
4–31 Phase I Completed (NCT02890069) Wang et al. (2018b)
Vorinostat (SAHA) Inline graphic PC-14
A549
A549-Oct4
H460-luc
Class I
Class IIa
Class IIb
HDAC-1
HDAC-2
HDAC-3
HDAC-8
HDAC-4
HDAC-7
HDAC-9
HDAC-6
81.7 ± 1.4
281.0 ± 2.2
32.8 ± 1.6
>10
20.0 ± 0.2
------
1975.0 ± 35.0
------
Phase I Completed (NCT01059552) Shieh et al. (2017)
CG347B Inline graphic A549
NCI-H460
NCI-H1299
Class IIb HDAC-6 5000 Not yet evaluated Wang et al. (2020b)
Pracinostat Inline graphic LU505, DMS53 Class I
Class IIa
Class IIb
Class IV
HDAC-1
HDAC-2
HDAC-3
HDAC-8
HDAC-4
HDAC-7
HDAC-9
HDAC-6
HDAC-11
125 Not yet evaluated Jia et al. (2018)
Trichostatin A (TSA) Inline graphic H1975
HCC827
A549
Class I
Class IIb
HDAC-1
HDAC-2
HDAC-3
HDAC-6
81.3
232
400
Not yet evaluated Tang et al. (2018), Meng et al. (2021)
CAY10603 Inline graphic A549
HCC827
H1975
C57BL/6 male mice
Class IIb HDAC-6 10, 5 mg/kg Not yet evaluated Liu et al., 2019, Wang et al. (2016c)
SNOH-3 Inline graphic A549
NCI-H1299
Class I HDAC-1 822 Not yet evaluated Wang et al. (2016a)
MPT0E028 Inline graphic A549
H1299
H1975
PC9/IR
CL97
Class I
Class IIb
HDAC-1
HDAC-2
HDAC-8
HDAC-6
1550 ± 140
1100 ± 20
1300 ± 130
1660 ± 410
1350 ± 110
Not yet evaluated Chen et al. (2013)
S11 Inline graphic A549 CDDP resistants
H460 CDDP resistants
H1299 CDDP resistants
Class I HDAC-1
HDAC-2
1380
2320
139O
Not yet evaluated Sun et al. (2019)
Mocetinostat Inline graphic H23
H1299
H1437
H1703
H1792
H1838
H2122
CT26
Class I HDAC-1
HDAC-2
HDAC-3
HDAC-8
1000 Phase II completed (NCT02954991) Briere et al. (2018)
Valproic acid (VPA) Inline graphic 1. A549 Class I
Class IIa
HDAC-1
HDAC-2
HDAC-3
HDAC-8
HDAC-4
HDAC-5
HDAC-7
HDAC-9
10.5
6.8 and 4.5
Phase I-II completed (NCT00084981, NCT00759824) Kalantar et al., 2021
CUDC-907 Inline graphic H196
SHP77
DMD273
H446
H526
H69
H82
DMS79
H2066
Class I
Class IIa
Class IIb
HDAC-1
HDAC-2
HDAC-3
HDAC-8
HDAC-4
HDAC-5
HDAC-7
HDAC-9
HDAC-6
HDAC-10
0.49
3.91
3.55
1.69
1.00
2.22
2.22
8.83
0.70
Not yet evaluated Ma et al. (2020)
Selisistat (EX527) Inline graphic A549
H1299
H157
DMS53 and Calu-1 cell lines
Class III SIRT 10,000
5000
Not yet evaluated Chen et al. (2017a), Guo et al. (2021)
YF454A Inline graphic A549
H1299
H1975 and PC9
150 to 3500 Not yet evaluated Yu et al. (2017)