TABLE 1

Summary of HDAC and DNMT inhibitors

Epigenetic ModifierClassificationCompoundChemical NameTarget
HDAC inhibitorsHydroxamatesSAHA (vorinostat)Pan inhibitor
PXD101 (belinostat)(E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamidePan inhibitor
LBH589 (panobinostat)(E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamideClasses I and II
ITF2357 (givinostat)[6-(diethylaminomethyl)naphthalen-2-yl]methyl-N-[4-(hydroxycarbamoyl)phenyl]carbamate;hydrate;hydrochloridePan inhibitor
4SC-201 (resminostat)(E)-3-[1-[4-[(dimethylamino)methyl]phenyl]sulfonylpyrrol-3-yl]-N-hydroxyprop-2-enamidePan inhibitor
PCI-24781 (abexinostat)3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamideClasses I and II
Cyclic peptidesDepsipeptide/FK228(1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentoneClass I
BenzamidesMS-275 (entinostat)N-[[4-[[(2-aminophenyl)amino]carbonyl]phenyl]methyl]-3-pyridinylmethyl ester, carbamic acidClass I
MGCD0103 (mocetinostat)N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamideClass I
M3444-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamideClass I
Aliphatic fatty acidsValproateClasses I and IIa
ButyrateClasses I and IIa
Unknown mechanismCI-9944-acetamido-N-(2-aminophenyl)benzamideHDAC1, HDAC2
BML-210N′-(2-aminophenyl)-N-phenyloctanediamideHDAC 1–5 and 7
NVP-LAQ824(E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamideUnknown
DNMT inhibitors5-AzacitidinePan inhibitor
5-aza-2′-deoxycytidinePan inhibitor
1-β-d-arabinofuranosyl-5-azacytosinePan inhibitor
Dihydro-5-azacytidinePan inhibitor
MG98DNMT1