Histone Methyltransferase Inhibitors

EZH1

EZH2

DOT1L

SMYD2

SMYD3

SUV39H2/KMT1B

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

SETDB1/KMT2G

SETD2/KMT3A

SETD7/KMT7

SETD8/KMT5A

PRMT1

PRMT3

PRMT4

PRMT5

PRMT6

PRMT7

PRMT8

Histone Methyltransferase Degraders & Inhibitors

Product Name	EZH1	EZH2	DOT1L	SMYD2	SMYD3	SUV39H2/KMT1B	EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D	SETDB1/KMT2G	SETD2/KMT3A	SETD7/KMT7	SETD8/KMT5A	PRMT1	PRMT3	PRMT4	PRMT5	PRMT6	PRMT7	PRMT8	Purity
GSK126		EZH2, IC₅₀: 9.9 nM																		99.98%
Pinometostat			DOT1L																	99.99%
Tazemetostat		EZH2																		99.93%
GSK3326595																PRMT5				99.97%
3-Deazaneplanocin A hydrochloride		EZH2																		99.98%
GSK343		EZH2																		99.88%
BIX-01294							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D												98.75%
Onametostat																PRMT5				99.79%
MS023													PRMT1	PRMT3			PRMT6		PRMT8	99.73%
UNC1999	EZH1	EZH2																		99.83%
UNC0379												SETD8/KMT5A								99.90%
UNC0224							G9a, IC₅₀: 15 nM G9a, Ki: 2.6 nM G9a, Kd: 23 nM	EHMT1/GLP/KMT1D, IC₅₀: 20-58 nM												99.31%
UNC0642							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D												99.92%
MRTX-1719																PRMT5				99.40%
SGC0946			DOT1L, IC₅₀: .3 nM																	99.68%
GSK591																PRMT5				99.87%
UNC0638							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D												99.71%
MS177		EZH2																		98.00%
A-366							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D												98.02%
TP-064															PRMT4, IC₅₀: <10 nM		PRMT6, IC₅₀: 1300 μM			98.35%
CM-272							G9a, IC₅₀: 8 nM	EHMT1/GLP/KMT1D, IC₅₀: 2 nM												99.27%
AMI-1													PRMT1							≥98.0%
SETDB1-TTD-IN-1									SETDB1/KMT2G											99.61%
LLY-283																PRMT5				99.22%
MS1943		EZH2, IC₅₀: 120 nM																		98.02%
SGC707														PRMT3, IC₅₀: 31 nM						98.08%
Valemetostat tosylate	EZH1																			98.14%
EPZ020411 hydrochloride													PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.15%
EZM0414										SETD2/KMT3A										99.45%
PFI-2 hydrochloride											SETD7/KMT7									99.52%
SGC3027																		PRMT7		98.29%
Valemetostat	EZH1																			99.65%
EPZ031686					SMYD3, IC₅₀: 3 nM															99.71%
EPZ011989		EZH2																		99.00%
EPZ-719										SETD2/KMT3A										99.85%
AZ505				SMYD2																99.99%
LLY-507				SMYD2, IC₅₀: <15 nM																98.28%
TNG908																PRMT5				98.89%
UNC 0631							G9a, IC₅₀: 4 nM													98.35%
UNC0321							G9a, Ki: 63 pM G9a, IC₅₀: 6-9 nM	EHMT1/GLP/KMT1D, IC₅₀: 15-23 nM												99.80%
PROTAC EZH2 Degrader-1		EZH2, IC₅₀: 2.7 nM																		98.55%
SGC2085															PRMT4					99.45%
UNC0646							G9a, IC₅₀: 6 nM	GLP, IC₅₀: <15 nM												99.82%
GSK2807 Trifluoroacetate					SMYD3, Ki: 14 nM SMYD3, IC₅₀: 130 nM															99.36%
GSK503		EZH2																		99.52%
MRTX9768																PRMT5				99.60%
JQEZ5		EZH2																		98.08%
BAY-598				SMYD2																99.30%
MS023 dihydrochloride													PRMT1	PRMT3			PRMT6		PRMT8	99.78%
EPZ020411													PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.06%
Furamidine dihydrochloride													PRMT1							≥99.0%
EPZ005687		EZH2, Ki: 24 nM																		99.79%
PF-06726304		EZH2 WT, Ki: 0.7 nM EZH2 Y641N, Ki: 3.0 nM																		98.37%
DS-437																PRMT5		PRMT7		98.00%
Gambogenic acid		EZH2																		99.94%
EI1		EZH2 Y641F mutant type, IC₅₀: 13 nM EZH2 WT, EC₅₀: 15 nM																		99.78%
BAY-6035					SMYD3, IC₅₀: 88 nM															99.82%
MS049															PRMT4, : 34 nM		PRMT6, : 43 nM		PRMT8, : 1600 nM	≥98.0%
MS117																	PRMT6			≥98.0%
DCLX069													PRMT1, IC₅₀: 17.9 μM							98.38%
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH		EZH2																		98.24%
PRMT5-IN-25																PRMT5, Ki: 0.06 nM				99.94%
BRD0639																PRMT5				99.17%
BRD9539							G9a, IC₅₀: 6.3 μM													99.74%
GNA002		EZH2, IC₅₀: 1.1 μM																		98.05%
EM127					SMYD3															98.37%
HLCL-61 hydrochloride																PRMT5				99.95%
SETDB1-TTD-IN-1 TFA									SETDB1/KMT2G											98.79%
EHMT2-IN-2							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM												≥99.0%
EZH2-IN-2		EZH2, IC₅₀: 64 nM																		99.40%
Dot1L-IN-5			DOT1L, IC₅₀: 0.17 nM																	98.57%
SMYD3-IN-1					SMYD3, IC₅₀: 11.7 nM															98.01%
NSC745885		EZH2																		≥98.0%
AZ506				SMYD2, IC₅₀: 17 nM																99.74%
OTS193320						SUV39H2/KMT1B														98.64%
EHMT2-IN-1							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM												99.85%
UNC2399		EZH2, IC₅₀: 17 nM																		99.62%
RK-701							G9a, IC₅₀: 23-27 nM													98.04%
PF-06939999																PRMT5				99.69%
MRTX-1719 hydrochloride																PRMT5				99.22%
Dot1L-IN-4			DOT1L, IC₅₀: 0.11 nM																	99.60%
MS8511							G9a, IC₅₀: 100 nM G9a, Kd: 44 nM	GLP, IC₅₀: 140 nM GLP, Kd: 46 nM
Tanshindiol C		EZH2, IC₅₀: 0.55 μM																		98.47%
EPZ011989 trifluoroacetate		EZH2																		98.71%
(S)-HH2853		EZH2 Y641N, IC₅₀: <100 nM
ZZM-1220							G9a, IC₅₀: 458 nM	GLP, IC₅₀: 924 nM												98.74%
Tulmimetostat	EZH1	EZH2
CARM1-IN-1 hydrochloride															PRMT4
(R)-HH2853		EZH2 Y641F mutant type, IC₅₀: <100 nM
DW14800																PRMT5				99.63%
PRMT5-IN-1																PRMT5
EML741							G9a, IC₅₀: 23 nM G9a, Kd: 1.13 μM
Dot1L-IN-1 TFA			DOT1L																	98.56%
NUCC-0226272		EZH2
PRMT5-IN-4																PRMT5
PRMT5-IN-30																PRMT5, IC₅₀: 0.33 μM PRMT5, Kd: 0.987 μM
BIX-01294 hydrochloride hydrate							G9a, IC₅₀: 1.7 μM	GLP, IC₅₀: 38 μM
CPI-1328		EZH2
Dot1L-IN-1			DOT1L
PRMT5-IN-14																PRMT5
GSK3368715 trihydrochloride													PRMT1, IC₅₀: 3.1 nM	PRMT3, IC₅₀: 48 nM	PRMT4, IC₅₀: 1148 nM		PRMT6, IC₅₀: 5.8 nM		PRMT8, IC₅₀: 1.7 nM
PF-06726304 acetate		EZH2 WT, Ki: 0.7 nM EZH2 Y641N, Ki: 3.0 nM
3-Deazaneplanocin A hydrochloride (GMP)		EZH2
IHMT-EZH2-426		EZH2 WT, IC₅₀: 1.3 nM EZH2-A687V, IC₅₀: 1.2 nM Y641F/Y641N/Y641S, IC₅₀: 1.7-3.5 nM
BBDDL2059		EZH2 Y641F mutant type, IC₅₀: 1.5 nM
EZH2-IN-4		WT 5-mer EZH2, IC₅₀: 0.923 nM mut 5-mer EZH2, IC₅₀: 2.65 nM
EZH2/HSP90-IN-29		EZH2, IC₅₀: 6.29 nM
PRMT5-IN-28																PRMT5
PRMT4-IN-1													PRMT1, IC₅₀: 0.835 μM	PRMT3, IC₅₀: 4.05 μM	PRMT4, IC₅₀: 3.2 nM	PRMT5, IC₅₀: 1.46 μM	PRMT6, IC₅₀: 1.75 μM	PRMT7, IC₅₀: 1.68 μM	PRMT8, IC₅₀: 1.95 μM
CSV0C018875							G9a
DM-01		EZH2																		98.03%
PARP/EZH2-IN-2		EZH2, IC₅₀: 27.34 ± 1. nM
PRMT5-IN-19													PRMT1, IC₅₀: 3.252 μM		PRMT4, IC₅₀: >20 μM	PRMT5, IC₅₀: 23.9 nM
MS8847		EZH2
EZH2-IN-5		EZH2 WT, IC₅₀: 1.52 nM EZH2 Y641F mutant type, IC₅₀: 4.07 nM
Antitumor agent-101							G9a, IC₅₀: 8.5 nM	GLP, IC₅₀: 5.5 nM
SMYD3-IN-2					SMYD3, IC₅₀: 0.81 μM μM
PARP/EZH2-IN-1		EZH2, IC₅₀: 36.51 nM
YM458		EZH2, IC₅₀: 490 nM
(S)-MRTX-1719																PRMT5
PRMT5-IN-9																PRMT5, IC₅₀: 0.01 μM
CARM1-IN-4													PRMT1, IC₅₀: 56 nM	PRMT3, IC₅₀: 2637 nM		PRMT5, IC₅₀: >100,000 nM	PRMT6, IC₅₀: 30 nM		PRMT8, IC₅₀: 31 nM
Dot1L-IN-7			DOT1L, IC₅₀: 1 μM
PRMT5-IN-23																PRMT5
UNC2327														PRMT3						99.70%
DCG066							G9a
PRMT5-IN-33													PRMT1, IC₅₀: 6.89 μM			PRMT5, IC₅₀: 10.9 nM
PRMT5-IN-21																PRMT5
MU1656			DOT1L, IC₅₀: 2 nM
SGC2085 hydrochloride																	PRMT6, IC₅₀: 5.2 μM

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