Histone Methyltransferase Inhibitors

EZH1

EZH2

DOT1L

SMYD2

SMYD3

SUV39H2/KMT1B

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

ASH1L/KMT2H

SETDB1/KMT2G

SETD2/KMT3A

NSD2/MMSET/WHSC1

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	ASH1L/KMT2H	SETDB1/KMT2G	SETD2/KMT3A	NSD2/MMSET/WHSC1	SETD7/KMT7	SETD8/KMT5A	PRMT1	PRMT3	PRMT4	PRMT5	PRMT6	PRMT7	PRMT8	Purity
Tazemetostat		EZH2																				99.93%
GSK126		EZH2, IC₅₀: 9.9 nM																				99.98%
Pinometostat			DOT1L																			99.99%
GSK3326595																		PRMT5				99.83%
GSK343		EZH2																				99.46%
CDK9/EZH2-IN-1		EZH2, IC₅₀: 108.6 nM
3-Deazaneplanocin A hydrochloride		EZH2																				99.98%
Navlimetostat																		PRMT5				99.40%
BIX-01294							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D														98.44%
EZM0414 TFA											SETD2/KMT3A
UNC0642							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D														99.86%
3-Deazaneplanocin A		EZH2																				99.97%
Valemetostat	EZH1																					99.84%
EPZ004777			DOT1L																			99.00%
UNC1999	EZH1	EZH2																				99.87%
EPZ015666																		PRMT5				99.83%
UNC0638							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D														99.48%
MS023															PRMT1	PRMT3			PRMT6		PRMT8	99.93%
GSK3368715 dihydrochloride															PRMT1	PRMT3	PRMT4		PRMT6		PRMT8	99.96%
Onametostat																		PRMT5				99.83%
SGC0946			DOT1L, IC₅₀: 0.3 nM																			99.68%
GSK591																		PRMT5				99.91%
UNC0379														SETD8/KMT5A								99.17%
A-366							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D														98.01%
SGC707																PRMT3, IC₅₀: 31 nM						99.71%
MS177		EZH2																				99.55%
TP-064																	PRMT4, IC₅₀: <10 nM		PRMT6, IC₅₀: 1300 μM			99.61%
MS1943		EZH2 methyltransferase, IC₅₀: 120 nM																				98.92%
EZM0414											SETD2/KMT3A											99.11%
UNC0224							G9a, IC₅₀: 15 nM G9a, Ki: 2.6 nM G9a, Kd: 23 nM	EHMT1/GLP/KMT1D, IC₅₀: 20-58 nM														98.85%
SGC3027																				PRMT7		98.06%
SETDB1-TTD-IN-1										SETDB1/KMT2G												99.93%
EPZ020411															PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.07%
CM-272							G9a, IC₅₀: 8 nM	EHMT1/GLP/KMT1D, IC₅₀: 2 nM														98.70%
LLY-283																		PRMT5				99.22%
PFI-2 hydrochloride													SETD7/KMT7									99.48%
Ralometostat																		PRMT5				99.90%
A-395		EZH2																				99.12%
AS-99 TFA									ASH1L/KMT2H													99.15%
AMI-1															PRMT1							98.0%
Valemetostat tosylate	EZH1																					99.84%
BCI-121					SMYD3																	99.89%
EPZ-719											SETD2/KMT3A											99.00%
TC-E 5003															PRMT1							98.03%
PROTAC EZH2 Degrader-1		EZH2, IC₅₀: 2.7 nM																				99.44%
Furamidine dihydrochloride															PRMT1							99.0%
LLY-507				SMYD2, IC₅₀: <15 nM																		98.47%
UNC 0631							G9a, IC₅₀: 4 nM															99.27%
EPZ031686					SMYD3, IC₅₀: 3 nM																	99.71%
PF-06939999																		PRMT5				99.84%
AZ505				SMYD2																		99.99%
BVT948														SETD8/KMT5A								≥99.0%
Tulmimetostat	EZH1	EZH2																				99.79%
EPZ020411 hydrochloride															PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.15%
EPZ011989		EZH2																				98.79%
BAY-598				SMYD2																		99.33%
Gambogenic acid		EZH2																				99.91%
UNC0321							G9a, Ki: 63 pM G9a, IC₅₀: 6-9 nM	EHMT1/GLP/KMT1D, IC₅₀: 15-23 nM														99.91%
SGC2085																	PRMT4					99.46%
BRD4770							EHMT2/G9a/KMT1C															99.69%
RK-701							G9a, IC₅₀: 23-27 nM															98.04%
PF-06726304		EZH2 WT, Ki: 0.7 nM EZH2 Y641N, Ki: 3.0 nM																				99.71%
EPZ005687		EZH2, Ki: 24 nM																				99.46%
Dot1L-IN-4			DOT1L, IC₅₀: 0.11 nM																			99.67%
MS4322	EZH1	EZH2	DOT1L	SMYD2	SMYD3	SUV39H2/KMT1B	EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D		SETDB1/KMT2G	SETD2/KMT3A	NSD2	SETD7/KMT7	SETD8/KMT5A	PRMT1	PRMT3	PRMT4	PRMT5	PRMT6	PRMT7	PRMT8	99.14%
MS023 dihydrochloride															PRMT1	PRMT3			PRMT6		PRMT8	99.68%
GSK3368715															PRMT1	PRMT3	PRMT4		PRMT6		PRMT8	99.19%
MS117																			PRMT6			98.0%
LLC0424												NSD2, DC₅₀: 20 nM										98.42%
JQEZ5		EZH2																				98.14%
NUCC-0226272		EZH2																				99.68%
C-7280948															PRMT1							99.91%
CARM1-IN-1																	PRMT4
MS8847		EZH2																				99.78%
GSK503		EZH2																				99.52%
AM-9747																		PRMT5, Ki: 0.06 nM				99.94%
MRTX9768																		PRMT5				99.60%
DCLX069															PRMT1, IC₅₀: 17.9 μM							98.03%
DS-437																		PRMT5		PRMT7		99.22%
EI1		EZH2 Y641F mutant type, IC₅₀: 13 nM EZH2 WT, EC₅₀: 15 nM																				99.78%
UNC0646							G9a, IC₅₀: 6 nM	GLP, IC₅₀: <15 nM														99.38%
AS-85									ASH1L/KMT2H													98.05%
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH		EZH2																				99.06%
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%
LEM-14												NSD2, IC₅₀: 132 μM										98.02%
HLCL-61 hydrochloride																		PRMT5				99.87%
MS049																	PRMT4, : 34 nM		PRMT6, : 43 nM		PRMT8, : 1600 nM	98.0%
GSK2807 Trifluoroacetate					SMYD3, Ki: 14 nM SMYD3, IC₅₀: 130 nM																	99.83%
AZ505 ditrifluoroacetate				SMYD2																		99.89%
BAY-6035					SMYD3, IC₅₀: 88 nM																	99.82%
EM127					SMYD3																	99.94%
PROTAC EZH2 Degrader-2		EZH2																				99.78%
Navlimetostat hydrochloride																		PRMT5				99.22%
BRD0639																		PRMT5				98.04%
PR5-LL-CM01																		PRMT5				98.37%
EPIC-0628		EZH2																				98.93%
MS8511							G9a, IC₅₀: 100 nM G9a, Kd: 44 nM	GLP, IC₅₀: 140 nM GLP, Kd: 46 nM
EZH2-IN-2		EZH2, IC₅₀: 64 nM																				98.51%
UNC2399		EZH2, IC₅₀: 17 nM																				99.62%
MS4322 (isomer)	EZH1	EZH2	DOT1L	SMYD2	SMYD3	SUV39H2/KMT1B	EHMT2/G9a/KMT1C	EHMTI PEP		SETDB1/KMT2G	SETD2/KMT3A	NSD2	SETD7/KMT7	SETD8/KMT5A	PRMT1	PRMT3	PRMT4	PRMT5	PRMT6	PRMT7	PRMT8	99.22%
NSD2-PWWP1-IN-1												NSD2, IC₅₀: 0.64 μM										98.72%
BRD9539							G9a, IC₅₀: 6.3 μM															99.73%
PRMT5-IN-30																		PRMT5, IC₅₀: 0.33 μM PRMT5, Kd: 0.987 μM				99.17%
CARM1-IN-1 hydrochloride																	PRMT4
CMP-5																		PRMT5				99.61%
EHMT2-IN-2							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM														99.0%
SGC8158																				PRMT7
NSD2-PWWP1-IN-3												NSD2, IC₅₀: 8.05 μM										99.63%
ZZM-1220							G9a, IC₅₀: 458 nM	GLP, IC₅₀: 924 nM														98.74%
EBI-2511		EZH2																				99.81%
Dot1L-IN-5			DOT1L, IC₅₀: 0.17 nM																			99.82%
DC-S239			DOT1L				EHMT2/G9a/KMT1C															99.73%
SETDB1-TTD-IN-1 TFA										SETDB1/KMT2G												99.77%
SMYD3-IN-1					SMYD3, IC₅₀: 11.7 nM																	98.01%
NSD2-PWWP1-IN-2												NSD2, IC₅₀: 1.49 μM										99.64%
DM-01		EZH2																				98.05%
Tanshindiol C		EZH2, IC₅₀: 0.55 μM																				98.47%
NSC745885		EZH2																				98.0%
YM458		EZH2, IC₅₀: 490 nM																				99.16%
W4275												NSD2, IC₅₀: 17 nM										98.93%
DW14800																		PRMT5				99.63%
CPUY074020							EHMT2/G9a/KMT1C															98.56%
GNA002		EZH2, IC₅₀: 1.1 μM																				98.02%
AZ506				SMYD2, IC₅₀: 17 nM																		99.74%
TDI-6118		EZH2																				99.08%
EPZ011989 trifluoroacetate		EZH2																				98.71%
(S)-HH2853		EZH2 Y641N, IC₅₀: <100 nM
A-893				SMYD2
PRMT5-IN-1																		PRMT5
AS-99 free base									ASH1L/KMT2H
EML741							G9a, IC₅₀: 23 nM G9a, Kd: 1.13 μM
MRTX9768 hydrochloride																		PRMT5				99.88%
PRMT5-IN-1 hydrochloride																		PRMT5				99.51%
Dot1L-IN-1 TFA			DOT1L																			98.56%
PFI-2													SETD7/KMT7
DCG066							G9a															99.78%
(R)-HH2853		EZH2 Y641F mutant type, IC₅₀: <100 nM
PRMT5-IN-4																		PRMT5				99.0%
BIX-01294 hydrochloride hydrate							G9a, IC₅₀: 1.7 μM	GLP, IC₅₀: 38 μM
CPI-1328		EZH2
AS-99									ASH1L/KMT2H
Dot1L-IN-1			DOT1L
CM112															PRMT1
PRT543																		PRMT5
SKLB-0124																			PRMT6, DC₅₀: 15.4 nM
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
PRMT5-MTA-IN-1																		PRMT5
PRMT5-IN-39-d₃																		PRMT5
EZH2-IN-22		EZH2 Y641N, IC₅₀: <0.00051 μM EZH2 Y641F mutant type, IC₅₀: <0.00051 μM EZH2 WT, IC₅₀: 0.00052 μM
BBDDL2059		EZH2 Y641F mutant type, IC₅₀: 1.5 nM
PRMT5-IN-34																		PRMT5
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
EZH2-IN-16		EZH2 WT, IC₅₀: 37.6 nM EZH2 Y641F mutant type, IC₅₀: 79.1 nM
Dot1L-IN-9			DOT1L, IC₅₀: 125 nM
HDACs/EZH2-IN-1		EZH2 WT, IC₅₀: 0.84 nM EZH2 Y641N, IC₅₀: 1.36 nM
PRMT5-IN-28																		PRMT5
PRMT5-IN-52																		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
PARP/EZH2-IN-2		EZH2, IC₅₀: 27.34 ± 1. nM
PRMT5-IN-47																		PRMT5, IC₅₀: 15 nM
PRMT5-IN-19															PRMT1, IC₅₀: 3.252 μM		PRMT4, IC₅₀: >20 μM	PRMT5, IC₅₀: 23.9 nM
EZH2-IN-5		EZH2 WT, IC₅₀: 1.52 nM EZH2 Y641F mutant type, IC₅₀: 4.07 nM
PRMT5-MTA-IN-4																		PRMT5, IC₅₀: 8 nM
SGC0946 TFA			DOT1L, IC₅₀: 0.3 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
PROTAC PRMT3 degrader 1																PRMT3
PRMT1-IN-3															PRMT1, IC₅₀: 4.11 μM	PRMT3, IC₅₀: > 100 μM	PRMT4, IC₅₀: > 100 μM	PRMT5, IC₅₀: > 100 μM	PRMT6, IC₅₀: 23.3 μM	PRMT7, IC₅₀: > 100 μM	PRMT8, IC₅₀: 30.1 μM
(S)-Navlimetostat																		PRMT5
PRMT5-IN-45																		PRMT5, IC₅₀: 3 nM
PRMT5-IN-43																		PRMT5
PRMT5-MTA-IN-5																		PRMT5, IC₅₀: 1.15 nM
PRMT3-IN-4																PRMT3
PRMT5-IN-44																		PRMT5
PRMT3-IN-5																PRMT3, IC₅₀: 261 nM
D-01		EZH2, IC₅₀: 0.99 μM
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
C199																	PRMT4
UNC2327																PRMT3						99.70%
EZH2-IN-7		EZH2
AMI-408															PRMT1
PRMT5-IN-49																		PRMT5, IC₅₀: > 100 μM
PRMT5-IN-33															PRMT1, IC₅₀: 6.89 μM			PRMT5, IC₅₀: 10.9 nM
PRMT5-IN-21																		PRMT5
PRMT5-IN-36-d₃																		PRMT5
EZH2-IN-19		EZH2 WT, IC₅₀: 0.32 nM EZH2 Y641F mutant type, IC₅₀: 0.03 nM EZH2 Y641N, IC₅₀: 0.08 nM
PRMT5-IN-53																		PRMT5, pIC₅₀: ≥ 9.7
MU1656			DOT1L, IC₅₀: 2 nM
SGC2085 hydrochloride																			PRMT6, IC₅₀: 5.2 μM
PROTAC G9a/GLP degrader 1							G9a, DC₅₀: 336 nM	GLP, DC₅₀: 988 nM
SKLB-03220		EZH2 WT, IC₅₀: 1.72 nM
EPZ0025654																			PRMT6, IC₅₀: 3 nM
GSK926		EZH2, IC₅₀: 0.02 μM
DCE_42		EZH2, IC₅₀: 22.6 μM

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