Table 2.

Types of epigenetic inhibitors used in pre-clinical and clinical trials for anti-cancer therapy

Inhibitor	Target	Tumor type/cell line	Trial phase [references]
HDAC inhibitors
Aliphatic acids	HDAC
Phenylbutyrate (PB)	Class I, IIa	AML, MDS, glioma	I [8, 9]
AN-9	Class I, IIa	NSCLC	II [10]
Valproic acid (VA)	Class I, IIa	Cervical cancer	I [11]
Sodium butyrate (SB)	Class I, IIa	Squamous cell carcinoma	Pre-clinical [12]
Benzamides
CI-994	Class I	Solid tumors	I [13]
MS-275	Class I	Solid tumors, lymphoma	I [14]
Cyclic peptides
Depsipeptidea	Class I	CLL, AML	I [15]
Apicidinb	Class I	Leukemia	Pre-clinical [16]
Hydroxamates
SAHA	Class I, IIa/b	Advanced cancer	I/II [17]
LAQ824, LBH589	Class I, IIa/b	Hematological cancer	I [18, 19]
Pyridoxine	Class I, IIa/b	Solid tumors	I [20]
PXD101	Class I, IIa/b	Solid tumors	I [21]
TSAc	Class I, IIa/b	Breast tumor	Pre-clinical [22]
CHAP compoundsd	Class I, IIa/b	Melanoma	Pre-clinical [23]
DNMT inhibitors
Nucleoside analog
5-Aza	DNMT-1, -3a, -3b	MDS	Approved [24]
Decitabine	DNMT-1, -3a, -3b	MDS, CML	II [25]
Gemcitabine	DNMT-1, -3a, -3b	Transitional cell carcinoma	I/II [26]
Zebularine	DNMT-1	Ovarian cancer	Pre-clinical [27]
Others
MG98	DNMT-1	Solid tumors	I [28]
Hydralazine	DNMT-1, -3a	Cervical cancer	I [29]
Procaine	DNMT-1	Breast tumor	Pre-clinical [30]
EGCGe	DNMT-1	Esophageal carcinoma	Pre-clinical [31]

^aIsolated from Chromobacterium

^bIsolated from two Fusarium species

^cIsolated from Streptomyces hygroscopicus

^dHybrid of TSA and trapoxin (isolated from Helicoma ambiens)

^eEpigallocatechin-3-gallate, the major polyphenol in green tea