Compound Isoform-Specificity Protein/enzyme/gene Cellular response Disease Reference
MS-275 HDACs 1,2,3,9 ↑Foxp3
↓nuclear NFκB p65, VEGF
↑IL-10
↓IL-1β, IFN-γ, IL-17, IL-18, TNF-α, IL-18, NO
RA [64,122]
MI192 HDAC3 ND ↓TNF, IL-6, IFN-γ RA [87]
MGCD0103 HDACs 1,2,3,11 Jak/STAT
↑NF-κB activation, TNFSF4, TNFSF9, TNF
TNFRSF8
↑TNF-α ND [79,80]
Valproic acid HDACs 1,2,3,8 PI3K/Akt, mTOR, NF-κB ↓TNF-α ALPS, SLE, IBD [52,78]
FK228 HDACs 1,2,3,4 ND ↓IL-1β, TNF-α AMA, RA, diabetes [20,88,89]
ACY-738 HDAC6 Foxp3 ↑TGF-β
↓IL-1β
SLE [117]
Unpublished data
Tubacin HDAC6 α-tubulin, HSp90 Foxp3
↑CTLA-4, PD-1, GITR
↓IL-2, IFN-γ
↑IL-10
RA, IBD [109,123]
Tubastatin A HDAC6 α-tubulin, Foxp3 ↓TNF-α, IL-6 RA, IBD [114,124]
ND: No data
Table 1: Isoform-Selective HDAC Inhibitors and Immune Regulation.