Histone Methyltransferase
Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.
DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.
Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.
Histone Methyltransferase Isoform Specific Products
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Histone Methyltransferase
(366)
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EZH1
(11)
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EZH2
(83)
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DOT1L
(21)
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SMYD2
(9)
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SMYD3
(9)
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SUV39H2/
KMT1B (4)View all products
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EHMT2/
G9a/ (32)KMT1C View all products
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EHMT1/
GLP/ (20)KMT1D View all products
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ASH1L/
KMT2H (4)View all products
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SETDB1/
KMT2G (4)View all products
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SETD2/
KMT3A (5)View all products
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NSD2/
MMSET/ (16)WHSC1 View all products
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NSD3/
WHSC1L1 (4)View all products
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SETD7/
KMT7 (6)View all products
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SETD8/
KMT5A (5)View all products
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PRMT1
(24)
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PRMT3
(17)
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PRMT4
(19)
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PRMT5
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PRMT6
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PRMT7
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PRMT8
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All Product Categories
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Histone Methyltransferase Inhibitors
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Histone Methyltransferase Agonists
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Histone Methyltransferase Antagonists
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Histone Methyltransferase Activators
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Histone Methyltransferase Modulators
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Histone Methyltransferase Chemical
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Histone Methyltransferase Inducers
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Histone Methyltransferase Degraders
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Histone Methyltransferase Controls
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Histone Methyltransferase Ligands
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Histone Methyltransferase Related Products (680)
Related Products (680)
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Antibodies (84)
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Histone Methyltransferase Isoform Comparison
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GSK2807 Trifluoroacetate (Standard)
0 ImagesCat. No.: HY-104009ARCAS No.: 2245255-66-5GSK2807 Trifluoroacetate (Standard) is the analytical standard of GSK2807 Trifluoroacetate (HY-104009A). This product is intended for research and analytical applications. GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM.
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NSC 663284 (Standard)
0 ImagesCat. No.: HY-100034RCAS No.: 383907-43-5Synonyms: DA-3003-1 (Standard)NSC 663284 (Standard) is the analytical standard of NSC 663284 (HY-100034). This product is intended for research and analytical applications. NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
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BIX-01294 (Standard)
0 ImagesCat. No.: HY-10587RCAS No.: 935693-62-2BIX-01294 (Standard) is the analytical standard of BIX-01294 (HY-10587). This product is intended for research and analytical applications. BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
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GSK591 (Standard)
0 ImagesSynonyms: EPZ015866 (Standard); GSK3203591 (Standard)
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ssK36
0 ImagesCat. No.: HY-P10463ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency.
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Valemetostat (Standard)
0 ImagesCat. No.: HY-109108RCAS No.: 1809336-39-7Synonyms: DS-3201 (Standard)Valemetostat (Standard) is the analytical standard of Valemetostat (HY-109108). This product is intended for research and analytical applications. Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
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A-196 (Standard)
0 ImagesCat. No.: HY-100201RCAS No.: 1982372-88-2A-196 (Standard) is the analytical standard of A-196 (HY-100201). This product is intended for research and analytical applications. A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
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Pemrametostat (Standard)
0 ImagesSynonyms: GSK3326595 (Standard); EPZ015938 (Standard)GSK3326595 (Standard) is the analytical standard of GSK3326595 (HY-101563). This product is intended for research and analytical applications. GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
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BG47
0 ImagesCat. No.: HY-117583ACAS No.: 1628784-54-2BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research.
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PRMT1-IN-2
0 ImagesCat. No.: HY-111030CAS No.: 947508-41-0PRMT1-IN-2 (RM65) is a potent PRMT1 inhibitor with an IC50 of 55.4 μM. PRMT1-IN-2 shows histone hypomethylation in HepG2 cells.
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PR5-LL-CM01 (Standard)
0 ImagesCat. No.: HY-109963RCAS No.: 1005307-86-7PR5-LL-CM01 (Standard) is the analytical standard of PR5-LL-CM01 (HY-109963). This product is intended for research and analytical applications. PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.
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MS453
0 ImagesCat. No.: HY-116255CAS No.: 2059892-29-2MS453 is a potent and highly selective SETD8 inhibitor with an IC50 value of 804 nM. MS453 specifically modifies a cysteine residue close to the inhibitor binding site. MS453 is selective for 28 other methyltransferases. The crystal structure of MS453 reveals its binding mode to SETD8, providing an atomic-level view for the development of high-quality chemical probes for SETD8.
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AMI-1 free acid (Standard)
0 ImagesCat. No.: HY-18962ARCAS No.: 134-47-4AMI-1 (free acid) (Standard) is the analytical standard of AMI-1 (free acid). This product is intended for research and analytical applications. AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
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BIX-01294 trihydrochloride (Standard)
0 ImagesCat. No.: HY-108239RCAS No.: 1392399-03-9BIX-01294 trihydrochloride (Standard) is the analytical standard of BIX-01294 (trihydrochloride) (HY-108239). This product is intended for research and analytical applications. BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
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UNC-4219 TFA
0 ImagesCat. No.: HY-125655CAS No.: 1872382-50-7
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A-395 (Standard)
0 ImagesCat. No.: HY-101512RCAS No.: 2089148-72-9A-395 (Standard) is the analytical standard of A-395 (HY-101512). This product is intended for research and analytical applications. A-395, a chemical probe, is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
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(1-Nitroethene-1,2-diyl)dibenzene
0 ImagesSynonyms: alpha-Nitrostilbene; α-Nitrostilbene; NSC 385(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
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EPZ030456
0 ImagesCat. No.: HY-122223CAS No.: 1808011-23-5
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EZM 2302 (Standard)
0 ImagesCat. No.: HY-111109RCAS No.: 1628830-21-6EZM 2302 (Standard) is the analytical standard of EZM 2302 (HY-111109). This product is intended for research and analytical applications. EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression.
