Catalog

Histone Methyltransferase Histone methyltransferase

Inhibitors

Cat.No.	Name	Information
M10532	Tazemetostat hydrobromide	Tazemetostat (EPZ-6438) hydrobromide is a potent, selective and orally available EZH2 inhibitor.
M10495	AMI-1 disodium salt	AMI-1 is a potent and selective, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50 values of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide.
M10073	HLCL-61 hydrochloride	HLCL-61 hydrochloride is a potent and selective, first-in-class protein arginine methyltransferase 5 (PRMT5) inhibitor.
M9789	MS049	MS049 is a potent and selective inhibitor of PRMT4,6 with IC50 values of 34 nM and 43 nM, respectively.
M9449	PFI-2 hydrochloride	PFI-2 hydrochloride is a potent, highly selective and cell-active inhibitor of the methyltransferase activity of SETD7, with IC50 of 2 nM.
M9442	CM-272	CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies.
M9420	GSK3326595	GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
M9151	MI-503	MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM.
M9150	MI-463	MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM.
M9145	MI-2	MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM.
M9004	WDR5-0103	WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).
M9003	MS023	MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.
M8989	BIX-01294	BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM.
M8933	EPZ011989	EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646.
M8196	Sinefungin	Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N⁶-methyladenosine, suggesting a role in gene expression.
M7578	SGC0946	SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
M7509	UNC0642	UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
M7508	JQ-EZ-05	JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
M6336	3-Deazaneplanocin A hydrochloride	3-Deazaneplanocin A hydrochloride is a eZH2 histone methyltransferase inhibitor.
M6312	LLY-283	LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.
M6288	LLY-507	LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
M6177	SGC2085	SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
M6142	XY1	XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive.
M5412	Amodiaquin dihydrochloride dihydrate	Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.
M5186	CPI-360	CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM.
M5163	SGC707	SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
M5128	PFI-2	PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
M4954	EPZ015666	EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
M4804	GSK-503	GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
M3101	UNC0224	UNC0224 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 15 nM and 20 nM, respectively.
M2675	EPZ004777 hydrochloride	EPZ004777 hydrochloride is the hydrochloride salt of EPZ004777, which is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
M2358	3-Deazaneplanocin A	3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with K_i of 50 pM.
M2334	EPZ004777	EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM.
M2179	EPZ-5676	EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase.
M2024	BIX 01294 Trihydrochloride	BIX 01294 Trihydrochloride is a potent inhitor of G9a histone methyltransferase with IC50 of 2.7 μM.

Signaling Pathways

Product Type

Histone Methyltransferase Histone methyltransferase

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