Table 1.

Potent and selective drugs to inhibit chromatin regulators.

Molecule	Protein Target (s)	Associated Chromatin Feature	IC50/EC50	References
DNA methyltransferase (DNMT) inhibitors
guadecitabine (SGI-110)	DNMTs	DNA methylation	–	[41]
Zebularine	DNMTs	DNA methylation	–	[39,42,43]
5-azacytidine (Vidaza)	DNMT1, DNMT2, and RRM2	DNA methylation	–	[35]
decitabine (Dacogen)	DNMT1	DNA methylation	–	[36]
Topoisomerase inhibitors
doxorubicin	Type II topoisomerases	Topology	–	[44]
daunorubicin	Type II topoisomerases	Topology	–	[45]
ICRF-193	Type II topoisomerases	Topology	–	[46]
etoposide	Type II topoisomerases	Topology	–	[47]
Histone deacetylase (HDAC) inhibitors
MS-275	HDAC1-3	histone acetylation	510 nM	[48]
PCI-34051	HDAC8	Cytoplasmic	10 nM	[49]
ACY-1215	HDAC6	Cytoplasmic	5 nM	[50]
LBH589 (Panobinostat)	HDAC classes I, II, and IV	histone acetylation	5 nM	[51]
PXD101 (Belinostat)	HDAC classes I, II, and IV	histone acetylation	27 nM	[52]
FK228 (Romidepsin)	HDAC class I	histone acetylation	47 nM	[53,54]
Trichostatin A	HDAC classes I, II	histone acetylation	20 nM	[55]
SAHA (Vorinostat, Zolinza)	HDAC classes I, II, and IV	histone acetylation	10 nM	[56]
Histone acetyltransferase inhibitors
A-485	CBP (p300)	histone acetylation	3–10 nM	[57,58]
anacardic acid	p300, PCAF	histone acetylation	24 nM	[59]
Histone demethylase inhibitors
GSK-LSD1(ORY-1001)	LSD1 (KDM1A)	H3K4me, H3K9me	<5 nM	[60]
GSK-J1	JMJD3, UTX, JARID1B	H3K27me	9 µM	[61]
Histone methyltransferase inhibitors
MRK-740	PRDM9	H3K4me3	800 nM	SGC 1
SKI-73, SKI-72	PRMT4 (CARM1)	H3R17me	1.3 µM	SGC 1
SGC3027	PRMT7	H4R3me2	<2.5 nM	SGC 1
BAY-6035	SMYD3	H3K4me2,3, H4K5me	70 nM	SGC 1
PFI-5	SMYD2	H3K4me1,-2,-3	900 nM	SGC 1
LLY-283	PRMT5	H4R3me, H3R8me	25 nM	SGC 1
TP-064	PRMT4	H3R17me	43 nM	[62]
A-395	EED (PRC2 complex)	H3K27me2	90 nM	[63]
A-196	SUV420H1, SUV420H2	H4K20me	500 nM	[64]
GSK591	PRMT5	H4R3me, H3R8me	56 nM	[65]
MS049	PRMT4, PRMT6	H3R17me, H3R2me	970 nM	[66]
OICR-9429	WDR5 (interacts with KMT2A)	H3K4me	233 nM	[67]
UNC1999	EZH2 (PRC2 complex)	H3K27me3	124 nM	[68]
PFI-2	SETD7	H3K4me	100 nM	[69]
SGC0946	DOT1L	H3K79me	10 nM	[70]
GSK343	EZH2	H3K27me3	174 nM	[71]
GSK126	EZH2	H3K27me3	9.9 nM	[72]
EPZ-6438 (Tazemetostat)	EZH2	H3K27me3	11 nM	[73]
MI-463	MENIN (interacts with KMT2A)	H3K4me	15 nM	[74]
MI-503	MENIN	H3K4me	14 nM	[74]
Histone acetyl reader inhibitors
I-CBP112	CBP (p300)	H3K18ac	5 µM	[75]
L-Moses	PCAF (GCN5)	H3K9ac	126–600 nM	[76]
GSK4027	PCAF (GCN5)	presumed acetyl-lysine	60 nM	[77]
BAY-850	ATAD2	presumed acetyl-lysine	1 µM	[78]
GSK8814	ATAD2, ATAD2B	presumed acetyl-lysine	2.7 µM	[79]
GSK6853	BRPF1B	presumed acetyl-lysine	20 nM	[80]
TP-472	BRD9, BRD7	presumed acetyl-lysine	320 nM	[81,82]
BAY-229	BRD1, TAF1	presumed acetyl-lysine	<13 nM	[83]
I-BRD9	BRD9	presumed acetyl-lysine	159 nM	[84]
PFI-3	SMARCA4, SMARCA2, PBRM1 (BAF and PBAFcomplexes)	presumed acetyl-lysine	1 µM	[85]
(+)-JQ1	BRD4, BET family	presumed acetyl-lysine	33–77 nM	[86]
Histone methyl reader inhibitors
UNC1215	L3MBTL3	H3K20me	40 nM	[87]
UNC3866	CBX4/CBX7 (PRC1 complex)	H3K27me3	66 nM	[88]
Histone ubiquitin ligase inhibitor
PRT4165	RING1A, RING1B (RNF2), (PRC1 complex)	H2AK119ub	3.9 µM	[89]

¹ Reference unavailable at time of writing but molecule available through the Structural Genomics Consortium (SGC).