TABLE 2.
Structure HDAC inhibitors | In vitro tests NSCLC cell lines | HDAC class | HDAC isozyme | HDAC Inhibition IC50 (nM) | Clinical assays | Reference |
---|---|---|---|---|---|---|
Panobinostat (LBH-589) | 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) | 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 | A549 NCI-H460 NCI-H1299 |
Class IIb | HDAC-6 | 5000 | Not yet evaluated | Wang et al. (2020b) |
Pracinostat | 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) | 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 | 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 | A549 NCI-H1299 |
Class I | HDAC-1 | 822 | Not yet evaluated | Wang et al. (2016a) |
MPT0E028 | 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 | 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 | 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) | 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 | 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) | 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 | A549 H1299 H1975 and PC9 |
150 to 3500 | Not yet evaluated | Yu et al. (2017) |