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).

HDACi	HDAC1	HDAC2	HDAC3	HDAC8	Purified HDACs	Additional 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