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Histone Methyltransferase

Histone Methyltransferase

Catalog No.	Product Name	Application	Product Information
A11757 SALE	GSK126	EZH2 inhibitor	GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. Product Citations (3) Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635每646 PMID: 29917168 Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218 Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646每32655 PMID: 26360609
A15920 SALE	CPI-169	EZH2 inhibitor	CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
A15916	AMI-1	Hmt1p/PRMT1 Inhibitor	AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 uM and 8.8 uM for yeast Hmt1p and human PRMT1, respectively.
A15908	CPI-360	EZH1 inhibitor	CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
A14374 SALE	GSK591	PRMT5 inhibitor	GSK591 is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.
A12585 SALE	MS023	PRMT1 inhibitor	MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues.
A15549	GSK503	EZH2 Inhibitor	GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
A15544	EPZ011989	EZH2 Inhibitor	EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
A13166 SALE	UNC-1999	EZH2/EZH1 Inhibitor	UNC1999 is the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. Product Citations (1) Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
A11377	DZNep	EZH2 Inhibitor	3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase.
A15870	HLCL-61	PRMT5 Inhibitor	HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
A15928	WDR5-0103	WDR5 antagonist	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 M).
A12929	MI-2 (Menin-MLL inhibitor 2)	Menin-MLL interaction inhibitor	MI-2 (Menin-MLL inhibitor 2) specifically binds to Menin and inhibits Menin??s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein?Cmediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins.
A15450 SALE	SGC 707	PRMT3 Inhibitor	SGC 707 is a potent allosteric inhibitor of PRMT3 (IC50 = 50 nM) with >100-fold selectivity over other methyltransferases and other non-epigenetic targets.
A15813 SALE	LLY-507	SMYD2 inhibitor	LLY-507 is a cell-active, small molecule inhibitor of SMYD2 with IC50 of= 15 nM.
A15807	XY1	PRMT3 inhibitor	XY1 is a negative control of SGC 707 . SGC 707 (Adooq Catalog# A15450) is a potent, selective allosteric inhibitor of PRMT3 (IC50 = 50 nM).
A12947 SALE	UNC0638	G9a/GLP HMTase inhibitor	UNC0638 is an inhibitor of protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
A15487 SALE	UNC0642	G9a/GLP inhibitor	UNC0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM). It reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM). Displays modest brain penetration in vivo.
A15969 SALE	A-366	G9a/GLP inhibitor	A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM.
A11599	UNC3866	CBX4 /CBX7 chromodomains antagonist	UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
A16378	TC-E 5003	PRMT1 inhibitor	TC-E 5003 is a selective inhibitor of PRMT1 with IC50 value of 1.5 uM .
A16377	EPZ020411	PRMT6 inhibitor	EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
A16375	EPZ031686	SMYD3/ MEKK2 inhibitor	EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
A16357	CPI-1205	EZH2 inhibitor	CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.
A13169	AZ505 ditrifluoroacetate	SMYD2 inhibitor	AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).
A13061	AZ505	SMYD2 inhibitor	AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 μM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 μM); DOT1L(IC50>83.3 μM);EZH2(IC50>83.3 μM).
A12711	EI1	EZH2 inhibitor	EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.
A13282	UNC 2400	EZH1/EZH2 inhibitor	UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1.
A15388	UNC 0224	G9a inhibitor	UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay.
A14401	BRD4770	G9a inhibitor	BRD4770 is a novel histone methyltransferase inhibitor.
A13200	UNC0321	G9a HMTase inhibitor	UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date
A13110	Opicapone (BIA 9-1067)	COMT inhibitor	opicapone is a novel catechol-O-methyltransferase inhibitor
A13114 SALE	GSK343	EZH2 inhibitor	GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).
A13195	UNC0631	G9a inhibitor	UNC-0631 is a novel G9a inhibitor with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.
A13194 SALE	UNC0646	G9a/GLP HMTase inhibitor	UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively).
A12812	Chaetocin	SUV39H HMT Inhibitor	Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 = 0.8 μM). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.
A12735 SALE	EPZ-5676 (Pinometostat)	DOT1L Inhibitor‎	EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Product Citations (1) Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
A11763 SALE	BIX 01294	G9a/GLP HMT inhibitor	BIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor.
A12712 SALE	EPZ-6438 (Tazemetostat)	EZH2 inhibitor	EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Product Citations (1) Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646每32655 PMID: 26360609
A12983	EPZ004777	DOT1L inhibitor	EPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes.
A13947	3-deazaneplanocin A HCl (DZNep HCl)	EZH2 inhibitor	3-deazaneplanocin A, also known as DZNep, is a well-known histone methyltransferase inhibitor, which disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma.
A14320 SALE	UNC0379	SETD8 HMTase inhibitor	UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies.
A14315	MM-102	MLL1 inhibitor	MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM.
A14216 SALE	PFI-2	SETD7 inhibitor	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.
A14218	MI-3	menin-MLL interaction inhibitor	MI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
A13690 SALE	UNC 0638	G9a/GLP inhibitor	UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases.
A13876	C7280948	PRMT1 inhibitor	C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM.
A12941 SALE	SGC 0946	DOT1L inhibitor	SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells.
A12439	EPZ005687	EZH2 inhibitor	EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM)
A16405	Amodiaquine 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.

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Histone Methyltransferase

A11757 SALE

A15920 SALE

A15916

A15908

A14374 SALE

A12585 SALE

A15549

A15544

A13166 SALE

A11377

A15870

A15928

A12929

A15450 SALE

A15813 SALE

A15807

A12947 SALE

A15487 SALE

A15969 SALE

A11599

A16378

A16377

A16375

A16357

A13169

A13061

A12711

A13282

A15388

A14401

A13200

A13110

A13114 SALE

A13195

A13194 SALE

A12812

A12735 SALE

A11763 SALE

A12712 SALE

A12983

A13947

A14320 SALE

A14315

A14216 SALE

A14218

A13690 SALE

A13876

A12941 SALE

A12439

A16405

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