BioMed Research International / 2016 / Article / Tab 1

Review Article

HDAC Inhibitors as Epigenetic Regulators of the Immune System: Impacts on Cancer Therapy and Inflammatory Diseases

Table 1

Specificities and IC50s for Class I HDAC inhibitors (HDACi).

HDACiHDAC1HDAC2HDAC3HDAC8Purified HDACsAdditional HDACs

TSA (trichostatin A) nM [11]
 nM [38]
100–300 nM [33]
 nM [11]
 nM [38]
 nM [11]
100–300 nM [33]
~100–300 nM [33]
 nM [11]
 nM [2]
3.4 nM [39]
Active against Class II HDACs 
(HDAC4  nM, HDAC6  nM, HDAC7  nM, HDAC9  nM) [11] HDAC4  nM, HDAC6  nM [38]

SAHA (vorinostat) nM [40]
 nM [11]
 nM [11] nM [40]
 nM [11]
 nM [40]
 nM [11]
 nM [40]Activity against HDAC6 
HDAC6  nM [40]

MS-275 (entinostat) nM [40]
 nM [11]
~300 nM [33]
 nM [11] nM [40]
 nM [11]
~8000 nM [33]
>10,000 nM [11]
44,900 ± 18,100 nM [40]
>100,000 nM [33]
11,000 ± 1,800 nM [40]Minimal activity against Class II HDACs
HDAC6 >100,000 nM [40]
HDAC9  nM [11]

MGCD0103 (mocetinostat) nM [11]
 nM [40]
 nM [1]
 nM [11]
 nM [1]
 nM [40]
 nM [11]
 nM [1]
1850 ±  nM [40]
>10,000 nM [1, 11]
≥25,000 nM [40]Minimal activity against Class II HDACs
HDAC11  nM [1]

FK228 (romidepsin) nM [38]
4 nM [41]
 nM [38]40 nM [41]No documented activity against Class II HDACs

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