Histone Methyltransferase Inhibitors

EZH1

EZH2

DOT1L

SMYD2

SMYD3

SUV39H2/KMT1B

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

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	SETDB1/KMT2G	SETD2/KMT3A	NSD2/MMSET/WHSC1	SETD7/KMT7	SETD8/KMT5A	PRMT1	PRMT3	PRMT4	PRMT5	PRMT6	PRMT7	PRMT8	Purity
GSK126		EZH2, IC₅₀: 9.9 nM																			99.98%
Tazemetostat		EZH2																			99.93%
Pinometostat			DOT1L																		99.99%
GSK3326595																	PRMT5				99.83%
3-Deazaneplanocin A hydrochloride		EZH2																			99.98%
NSD2-PWWP1-IN-2											NSD2, IC₅₀: 1.49 μM										99.64%
NSD2-PWWP1-IN-1											NSD2, IC₅₀: 0.64 μM										98.72%
NSD2-PWWP1-IN-3											NSD2, IC₅₀: 8.05 μM
GSK343		EZH2																			99.88%
BIX-01294							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D													98.44%
Navlimetostat																	PRMT5				99.40%
UNC0642							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D													99.92%
EPZ015666																	PRMT5				99.83%
Onametostat																	PRMT5				99.79%
SGC0946			DOT1L, IC₅₀: .3 nM																		99.68%
MS023														PRMT1	PRMT3			PRMT6		PRMT8	99.73%
UNC1999	EZH1	EZH2																			99.83%
EPZ004777			DOT1L																		99.00%
UNC0638							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D													99.05%
3-Deazaneplanocin A		EZH2																			99.97%
MS177		EZH2																			98.00%
GSK591																	PRMT5				99.91%
TP-064																PRMT4, IC₅₀: <10 nM		PRMT6, IC₅₀: 1300 μM			99.61%
UNC0379													SETD8/KMT5A								99.90%
Valemetostat	EZH1																				99.84%
SGC707															PRMT3, IC₅₀: 31 nM						98.08%
UNC0224							G9a, IC₅₀: 15 nM G9a, Ki: 2.6 nM G9a, Kd: 23 nM	EHMT1/GLP/KMT1D, IC₅₀: 20-58 nM													98.85%
A-366							EHMT2/G9a/KMT1C	EHMT1/GLP/KMT1D													98.01%
EZM0414										SETD2/KMT3A											99.11%
SETDB1-TTD-IN-1									SETDB1/KMT2G												99.93%
CM-272							G9a, IC₅₀: 8 nM	EHMT1/GLP/KMT1D, IC₅₀: 2 nM													98.70%
MS1943		EZH2 methyltransferase, IC₅₀: 120 nM																			98.92%
A-395		EZH2																			99.12%
SGC3027																			PRMT7		98.06%
Ralometostat																	PRMT5				98.89%
LLY-283																	PRMT5				99.22%
PFI-2 hydrochloride												SETD7/KMT7									99.52%
AMI-1														PRMT1							≥98.0%
Valemetostat tosylate	EZH1																				99.84%
EPZ020411														PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.07%
EPZ-719										SETD2/KMT3A											99.85%
EPZ020411 hydrochloride														PRMT1, IC₅₀: 0.119 μM				PRMT6, IC₅₀: 0.01 μM		PRMT8, IC₅₀: 0.223 μM	98.15%
UNC0321							G9a, Ki: 63 pM G9a, IC₅₀: 6-9 nM	EHMT1/GLP/KMT1D, IC₅₀: 15-23 nM													99.91%
AZ505				SMYD2																	99.99%
BCI-121					SMYD3																99.26%
EPZ031686					SMYD3, IC₅₀: 3 nM																99.71%
LLY-507				SMYD2, IC₅₀: <15 nM																	98.28%
PROTAC EZH2 Degrader-1		EZH2, IC₅₀: 2.7 nM																			99.44%
UNC 0631							G9a, IC₅₀: 4 nM														98.35%
SGC2085																PRMT4					99.46%
EPZ011989		EZH2																			98.79%
TC-E 5003														PRMT1							98.03%
Furamidine dihydrochloride														PRMT1							≥99.0%
Gambogenic acid		EZH2																			99.94%
BVT948													SETD8/KMT5A								≥99.0%
BRD4770							EHMT2/G9a/KMT1C														99.69%
MS023 dihydrochloride														PRMT1	PRMT3			PRMT6		PRMT8	99.30%
JQEZ5		EZH2																			98.08%
EPZ005687		EZH2, Ki: 24 nM																			99.46%
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	98.49%
MS117																		PRMT6			≥98.0%
PF-06726304		EZH2 WT, Ki: 0.7 nM EZH2 Y641N, Ki: 3.0 nM																			98.37%
PF-06939999																	PRMT5				99.69%
BAY-598				SMYD2																	99.30%
C-7280948														PRMT1							98.57%
GSK503		EZH2																			99.52%
CARM1-IN-1																PRMT4
RK-701							G9a, IC₅₀: 23-27 nM														98.04%
Dot1L-IN-4			DOT1L, IC₅₀: 0.11 nM																		99.54%
EI1		EZH2 Y641F mutant type, IC₅₀: 13 nM EZH2 WT, EC₅₀: 15 nM																			99.78%
MRTX9768																	PRMT5				99.60%
UNC0646							G9a, IC₅₀: 6 nM	GLP, IC₅₀: <15 nM													99.38%
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH		EZH2																			99.06%
MS049																PRMT4, : 34 nM		PRMT6, : 43 nM		PRMT8, : 1600 nM	≥98.0%
GSK2807 Trifluoroacetate					SMYD3, Ki: 14 nM SMYD3, IC₅₀: 130 nM																99.36%
BAY-6035					SMYD3, IC₅₀: 88 nM																99.82%
Tulmimetostat	EZH1	EZH2																			99.79%
LLC0424											NSD2, DC₅₀: 20 nM										98.42%
NUCC-0226272		EZH2																			99.68%
OTS193320						SUV39H2/KMT1B															98.64%
EM127					SMYD3																98.37%
PRMT5-IN-25																	PRMT5, Ki: 0.06 nM				99.94%
DCLX069														PRMT1, IC₅₀: 17.9 μM							98.03%
HLCL-61 hydrochloride																	PRMT5				99.87%
DS-437																	PRMT5		PRMT7		98.00%
BRD0639																	PRMT5				98.04%
AZ505 ditrifluoroacetate				SMYD2																	99.91%
EHMT2-IN-2							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM													≥99.0%
BRD9539							G9a, IC₅₀: 6.3 μM														99.74%
Navlimetostat hydrochloride																	PRMT5				99.22%
EHMT2-IN-1							EHMT2 PEP, IC₅₀: <100 nM EHMT2 ICW, IC₅₀: <100 nM	EHMTI PEP, IC₅₀: <100 nM													99.85%
MS8511							G9a, IC₅₀: 100 nM G9a, Kd: 44 nM	GLP, IC₅₀: 140 nM GLP, Kd: 46 nM
MS8847		EZH2																			99.78%
Dot1L-IN-5			DOT1L, IC₅₀: 0.17 nM																		98.57%
SMYD3-IN-1					SMYD3, IC₅₀: 11.7 nM																98.01%
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%
EPIC-0628		EZH2																			98.93%
EZH2-IN-2		EZH2, IC₅₀: 64 nM																			99.40%
CMP-5																	PRMT5				99.02%
GNA002		EZH2, IC₅₀: 1.1 μM																			98.02%
Tanshindiol C		EZH2, IC₅₀: 0.55 μM																			98.47%
PR5-LL-CM01																	PRMT5				98.45%
EBI-2511		EZH2																			99.81%
GSK3368715														PRMT1	PRMT3	PRMT4		PRMT6		PRMT8	99.24%
DC-S239			DOT1L				EHMT2/G9a/KMT1C														99.43%
SETDB1-TTD-IN-1 TFA									SETDB1/KMT2G												99.77%
NSC745885		EZH2																			≥98.0%
AZ506				SMYD2, IC₅₀: 17 nM																	99.74%
ZZM-1220							G9a, IC₅₀: 458 nM	GLP, IC₅₀: 924 nM													98.74%
PRMT5-IN-30																	PRMT5, IC₅₀: 0.33 μM PRMT5, Kd: 0.987 μM				99.17%
EPZ011989 trifluoroacetate		EZH2																			98.71%
DW14800																	PRMT5				99.63%
CPUY074020							EHMT2/G9a/KMT1C														98.56%
MRTX9768 hydrochloride																	PRMT5				99.88%
Dot1L-IN-1 TFA			DOT1L																		98.56%
YM458		EZH2, IC₅₀: 490 nM																			99.16%
CARM1-IN-1 hydrochloride																PRMT4
(S)-HH2853		EZH2 Y641N, IC₅₀: <100 nM
A-893				SMYD2
PRMT5-IN-1																	PRMT5
EML741							G9a, IC₅₀: 23 nM G9a, Kd: 1.13 μM
PRMT5-IN-1 hydrochloride																	PRMT5				99.50%
SGC8158																			PRMT7
PRMT5-IN-4																	PRMT5				≥99.0%
TDI-6118		EZH2
(R)-HH2853		EZH2 Y641F mutant type, IC₅₀: <100 nM
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
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
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-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
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
W4275											NSD2, IC₅₀: 17 nM
(S)-Navlimetostat																	PRMT5
PRMT5-IN-45																	PRMT5, IC₅₀: 3 nM
PRMT5-IN-43																	PRMT5
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
UNC2327															PRMT3						99.70%
DCG066							G9a														99.78%
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
MU1656			DOT1L, IC₅₀: 2 nM
SGC2085 hydrochloride																		PRMT6, IC₅₀: 5.2 μM
EPZ0025654																		PRMT6, IC₅₀: 3 nM
GSK926		EZH2, IC₅₀: 0.02 μM
DCE_42		EZH2, IC₅₀: 22.6 μM

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