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

NSD3/WHSC1L1

SETD7/KMT7

SETD8/KMT5A

PRMT1

PRMT3

PRMT4

PRMT5

PRMT6

PRMT7

PRMT8

Histone Methyltransferase Inhibitors, Modulators, Degraders, Controls & Ligands

Product Name	EZH1	EZH2	DOT1L	SMYD2	SMYD3	SUV39H2/KMT1B	EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D	ASH1L/KMT2H	SETDB1/KMT2G	SETD2/KMT3A	NSD2/MMSET/WHSC1	NSD3/WHSC1L1	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																					99.85%
EZM8266							G9a, IC₅₀: 1 pM																98.24%
YZ-836P																			PRMT5
Navlimetostat																			PRMT5				99.28%
EZM0414 TFA											SETD2/KMT3A
3-Deazaneplanocin A		EZH2																					99.97%
BIX-01294							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D															98.44%
Valemetostat	EZH1																						99.84%
UNC0642							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D															99.86%
3-Deazaneplanocin A hydrochloride		EZH2																					99.98%
EPZ004777			DOT1L																				99.74%
UNC0638							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D															99.84%
EPZ015666																			PRMT5				99.86%
UNC1999	EZH1	EZH2																					99.87%
Onametostat																			PRMT5				99.79%
MS023																PRMT1	PRMT3			PRMT6		PRMT8	99.93%
SGC0946			DOT1L, IC₅₀: 0.3 nM																				99.68%
UNC0379															SETD8/KMT5A								99.17%
GSK3368715 dihydrochloride																PRMT1	PRMT3	PRMT4		PRMT6		PRMT8	99.96%
SGC707																	PRMT3, IC₅₀: 31 nM						99.99%
A-366							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D															98.13%
GSK591																			PRMT5				99.91%
MS1943		EZH2 methyltransferase, IC₅₀: 120 nM																					98.92%
TP-064																		PRMT4, IC₅₀: <10 nM		PRMT6, IC₅₀: 1300 μM			99.29%
MS177		EZH2																					99.55%
EZM0414											SETD2/KMT3A												99.11%
SGC3027																					PRMT7		98.06%
LLY-283																			PRMT5				98.93%
CM-272							G9a, IC₅₀: 8 nM	EHMT1/GLP/KMT1D, IC₅₀: 2 nM															98.70%
EPZ020411																PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.07%
A-395		EZH2																					99.12%
PFI-2 hydrochloride														SETD7/KMT7									99.48%
UNC0224							G9a, IC₅₀: 15 nM G9a, Ki: 2.6 nM G9a, Kd: 23 nM	EHMT1/GLP/KMT1D, IC₅₀: 20-58 nM															98.93%
SETDB1-TTD-IN-1										SETDB1/KMT2G													99.93%
Valemetostat tosylate	EZH1																						99.84%
Ralometostat																			PRMT5				99.90%
PF-06939999																			PRMT5				99.84%
AMI-1																PRMT1							98.0%
AS-99 TFA									ASH1L/KMT2H														98.89%
EPZ020411 hydrochloride																PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.15%
Tulmimetostat	EZH1	EZH2																					99.79%
LLY-507				SMYD2, IC₅₀: <15 nM																			99.09%
AZ505				SMYD2																			99.99%
EPZ-719											SETD2/KMT3A												99.00%
TC-E 5003																PRMT1							98.06%
PROTAC EZH2 Degrader-1		EZH2, IC₅₀: 2.7 nM																					99.44%
Furamidine dihydrochloride																PRMT1							≥99.0%
UNC 0631							G9a, IC₅₀: 4 nM																99.27%
BRD4770							EHMT2/G9a/KMT1C																99.79%
MS8847		EZH2																					99.78%
GSK3368715																PRMT1	PRMT3	PRMT4		PRMT6		PRMT8	99.41%
LLC0424												NSD2, DC₅₀: 20 nM											98.41%
Dot1L-IN-4			DOT1L, IC₅₀: 0.11 nM																				99.67%
RK-701							G9a, IC₅₀: 23-27 nM																98.01%
EPZ031686					SMYD3, IC₅₀: 3 nM																		99.71%
PF-06726304		EZH2 WT, Ki: 0.7 nM EZH2 Y641N, Ki: 3.0 nM																					99.71%
EPZ011989		EZH2																					98.79%
Gambogenic acid		EZH2																					99.91%
BAY-598				SMYD2																			99.33%
BCI-121					SMYD3																		99.89%
BVT948															SETD8/KMT5A								≥99.0%
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%
EPZ005687		EZH2, Ki: 24 nM																					99.46%
SGC2085																		PRMT4					99.46%
NUCC-0226272		EZH2																					99.68%
UNC0321							G9a, Ki: 63 pM G9a, IC₅₀: 6-9 nM	EHMT1/GLP/KMT1D, IC₅₀: 15-23 nM															99.91%
LEM-14												NSD2, IC₅₀: 132 μM											98.02%
CARM1-IN-1																		PRMT4
MS117																				PRMT6			98.0%
DCLX069																PRMT1, IC₅₀: 17.9 μM							98.03%
EHMT2-IN-1							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM															99.85%
AS-85									ASH1L/KMT2H														98.05%
BAY-6035					SMYD3, IC₅₀: 88 nM																		99.51%
DS-437																			PRMT5		PRMT7		99.22%
EPZ004777 hydrochloride			DOT1L																				98.92%
EM127					SMYD3																		99.94%
5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide		EZH2																					98.22%
AZ505 ditrifluoroacetate				SMYD2																			99.89%
UNC0646							G9a, IC₅₀: 6 nM	GLP, IC₅₀: <15 nM															99.38%
HLCL-61 hydrochloride																			PRMT5				99.87%
JQEZ5		EZH2																					98.14%
MS049																		PRMT4, : 34 nM		PRMT6, : 43 nM		PRMT8, : 1600 nM	98.0%
C-7280948																PRMT1							99.91%
Dot1L-IN-5			DOT1L, IC₅₀: 0.17 nM																				99.82%
MRTX9768																			PRMT5				99.60%
OTS193320						SUV39H2/KMT1B																	98.12%
GSK503		EZH2																					99.52%
BRD0639																			PRMT5				98.04%
W4275												NSD2, IC₅₀: 17 nM											98.93%
PROTAC EZH2 Degrader-2		EZH2																					98.77%
Navlimetostat hydrochloride																			PRMT5				99.61%
EI1		EZH2 Y641F mutant type, IC₅₀: 13 nM EZH2 WT, EC₅₀: 15 nM																					98.84%
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH		EZH2																					99.06%
CARM1-IN-1 hydrochloride																		PRMT4
GSK2807 Trifluoroacetate					SMYD3, Ki: 14 nM SMYD3, IC₅₀: 130 nM																		99.83%
AM-9747																			PRMT5, Ki: 0.06 nM				99.76%
EPIC-0628		EZH2																					98.93%
SGC8158																					PRMT7
PR5-LL-CM01																			PRMT5				98.37%
PFI-2														SETD7/KMT7									99.68%
PRMT5-IN-30																			PRMT5, IC₅₀: 0.33 μM PRMT5, Kd: 0.987 μM				99.35%
AZ506				SMYD2, IC₅₀: 17 nM																			99.74%
NSD2-PWWP1-IN-1												NSD2, IC₅₀: 0.64 μM											98.72%
(S)-Navlimetostat																			PRMT5				98.15%
SMYD3-IN-1					SMYD3, IC₅₀: 11.7 nM																		98.03%
EHMT2-IN-2							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM															99.0%
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	99.87%
EZH2-IN-13		EZH2																					99.72%
NSD2-PWWP1-IN-2												NSD2, IC₅₀: 1.49 μM											99.64%
NSD2-PWWP1-IN-3												NSD2, IC₅₀: 8.05 μM											99.63%
TDI-6118		EZH2																					99.08%
EZH2-IN-2		EZH2, IC₅₀: 64 nM																					98.51%
CMP-5																			PRMT5				99.61%
GNA002		EZH2, IC₅₀: 1.1 μM																					98.02%
DC-S239			DOT1L				EHMT2/G9a/KMT1C																99.73%
SETDB1-TTD-IN-1 TFA										SETDB1/KMT2G													99.77%
CDK9/EZH2-IN-1		EZH2, IC₅₀: 108.6 nM																					99.08%
DM-01		EZH2																					98.05%
NSC745885		EZH2																					98.0%
Dot1L-IN-1 TFA			DOT1L																				99.59%
YM458		EZH2, IC₅₀: 490 nM																					99.16%
BRD9539							G9a, IC₅₀: 6.3 μM																99.73%
ZZM-1220							G9a, IC₅₀: 458 nM	GLP, IC₅₀: 924 nM															98.74%
EBI-2511		EZH2																					98.67%
DW14800																			PRMT5				99.12%
CPUY074020							EHMT2/G9a/KMT1C																98.56%
PRMT5-IN-1 hydrochloride																			PRMT5				99.51%
UNC2399		EZH2, IC₅₀: 17 nM																					99.16%
MS8511							G9a, IC₅₀: 100 nM G9a, Kd: 44 nM	GLP, IC₅₀: 140 nM GLP, Kd: 46 nM
AMI-408																PRMT1
PROTAC G9a/GLP degrader 1							G9a, DC₅₀: 336 nM	GLP, DC₅₀: 988 nM															98.22%
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														98.57%
EML741							G9a, IC₅₀: 23 nM G9a, Kd: 1.13 μM
MRTX9768 hydrochloride																			PRMT5				99.88%
AZD3470																			PRMT5				99.74%
Tanshindiol C		EZH2, IC₅₀: 0.55 μM																					98.47%
DOT1L808			DOT1L, DC₅₀: 5 nM
NSD2-IN-5												NSD2, IC₅₀: 0.001-0.01 μM
WX2-43																			PRMT5, Kd: 11.0 nM				98.74%
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
NSD2/H3K36me2 modulator-1												NSD2
PRMT5-IN-39-d₃																			PRMT5
MC4491																			PRMT5, IC₅₀: 0.043 μM
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
RAPRMT5																			PRMT5
AK442																		PRMT4
PARP1/EZH2-IN-1		EZH2, IC₅₀: 74 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
EPZ020411 dihydrochloride																				PRMT6, IC₅₀: 0.010 μM
EZH2-IN-16		EZH2 WT, IC₅₀: 37.6 nM EZH2 Y641F mutant type, IC₅₀: 79.1 nM
PRMT1 ligand-1																PRMT1
Dot1L-IN-9			DOT1L, IC₅₀: 125 nM
EZH2 ligand-1		EZH2
PROTAC EZH2 Degrader-38		EZH2
NSD2-IN-6	EZH1, IC₅₀: 3.8 nM EZH1, IC₅₀: 274 nM
EZH2 ligand-4		EZH2
HDACs/EZH2-IN-1		EZH2 WT, IC₅₀: 0.84 nM EZH2 Y641N, IC₅₀: 1.36 nM
PROTAC EZH2 Degrader-9		EZH2
EZH2 ligand-3		EZH2
PROTAC EZH2 Degrader-26	EZH1, IC₅₀: 0.06 μM	EZH2, IC₅₀: 5.80 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
SKLB06329																				PRMT6, IC₅₀: 3.86 nM
T/E PPI-IN-1		EZH2
PARP/EZH2-IN-2		EZH2, IC₅₀: 27.34 ± 1. nM
PRMT5-IN-47																			PRMT5, IC₅₀: 15 nM
PROTAC EZH2 Degrader-27		EZH2
DC-S238														SETD7/KMT7
MS8815N		EZH2
SKLB06489																PRMT1, IC₅₀: 64.55 nM				PRMT6, IC₅₀: 4.21 nM		PRMT8, IC₅₀: 51.27 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
PROTAC EZH2 Degrader-44		EZH2
PRMT5 ligand 3																			PRMT5
PRMT5-MTA-IN-4																			PRMT5, IC₅₀: 8 nM
SGC0946 TFA			DOT1L, IC₅₀: 0.3 nM
EZH2 ligand-Linker Conjugate 1		EZH2
DOT1L ligand-2			DOT1L
DC-PRC2in-01		EZH2
PROTAC EZH2 Degrader-21		EZH2
Antitumor agent-101							G9a, IC₅₀: 8.5 nM	GLP, IC₅₀: 5.5 nM
PRMT5-IN-54																			PRMT5
SMYD3-IN-2					SMYD3, IC₅₀: 0.81 μM μM
PROTAC EZH2 Degrader-41		EZH2
PARP/EZH2-IN-1		EZH2, IC₅₀: 36.51 nM
PROTAC PRMT3 degrader 1																	PRMT3, DC₅₀: 2.566 μM
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
PRMT5-IN-45																			PRMT5, IC₅₀: 3 nM
PRMT5-IN-43																			PRMT5
PRMT5-MTA-IN-5																			PRMT5, IC₅₀: 1.15 nM
UNC10415667												NSD2, DC₅₀: 460 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%
NPD13668		EZH2
EZH2-IN-7		EZH2
PRMT5-IN-49																			PRMT5, IC₅₀: > 100 μM
EPZ004777 formate			DOT1L, : 0.4 nM
PRMT1 ligand-Linker Conjugate 1																PRMT1
PRMT5-IN-33																PRMT1, IC₅₀: 6.89 μM			PRMT5, IC₅₀: 10.9 nM
MS2928															SETD8/KMT5A, IC₅₀: 0.14 μM
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
SKLB-03220		EZH2 WT, IC₅₀: 1.72 nM
RK-0080552												NSD2
EPZ0025654																				PRMT6, IC₅₀: 3 nM
GSK926		EZH2, IC₅₀: 0.02 μM
DCE_42		EZH2, IC₅₀: 22.6 μM
BI-9321-C10-acid													NSD3

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