2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

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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:

Histone Methyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-142048
    BI-9466
    		Antagonist
    BI-9466 (Compound 2) is a nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd of 144 µM. BI-9466 is a negative control compound of BI-9321 (HY-114208). BI-9466 has no inhibitory activity against NSD3-PWWP1 domain by introduction of a much basic nitrogen heterocycle at the 5-position of BI-9321.
    BI-9466
  • HY-122532
    Fagaronine chloride
    Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection.
    Fagaronine chloride
  • HY-12707R
    Piribedil (Standard)
    		Inhibitor
    Piribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil (Standard)
  • HY-100846R
    JQEZ5 (Standard)
    		Inhibitor
    JQEZ5 (Standard) is the analytical standard of JQEZ5 (HY-100846). This product is intended for research and analytical applications. JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
    JQEZ5 (Standard)
  • HY-110093
    UNC0638 hydrate
    		Inhibitor
    UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.
    UNC0638 hydrate
  • HY-104009AR
    GSK2807 Trifluoroacetate (Standard)
    		Inhibitor
    GSK2807 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.
    GSK2807 Trifluoroacetate (Standard)
  • HY-100034R
    NSC 663284 (Standard)
    		Inhibitor
    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).
    NSC 663284 (Standard)
  • HY-172369
    CARM1/IKZF3 ligand 1
    		Inhibitor
    CARM1/IKZF3 ligand 1 is the inhibitor for CARM1 that can be used as the target protein ligand for synthesis of PROTAC CARM1/IKZF3 degrader-1 (HY-172368).
    CARM1/IKZF3 ligand 1
  • HY-10587R
    BIX-01294 (Standard)
    		Inhibitor
    BIX-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.
    BIX-01294 (Standard)
  • HY-100235R
    GSK591 (Standard)
    		Inhibitor
    GSK591 (Standard) is the analytical standard of GSK591 (HY-100235). This product is intended for research and analytical applications. GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
    GSK591 (Standard)
  • HY-P10463
    ssK36
    		Inhibitor
    ssK36 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.
    ssK36
  • HY-100201R
    A-196 (Standard)
    		Inhibitor
    A-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.
    A-196 (Standard)
  • HY-101563R
    GSK3326595 (Standard)
    		Inhibitor
    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.
    GSK3326595 (Standard)
  • HY-117583A
    BG47
    		Activator
    BG47 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.
    BG47
  • HY-111030
    PRMT1-IN-2
    		Inhibitor
    PRMT1-IN-2 (RM65) is a potent PRMT1 inhibitor with an IC50 of 55.4 μM. PRMT1-IN-2 shows histone hypomethylation in HepG2 cells.
    PRMT1-IN-2
  • HY-116255
    MS453
    MS453 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.
    MS453
  • HY-18962AR
    AMI-1 free acid (Standard)
    		Inhibitor
    AMI-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.
    AMI-1 free acid (Standard)
  • HY-108239R
    BIX-01294 trihydrochloride (Standard)
    		Inhibitor
    BIX-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.
    BIX-01294 trihydrochloride (Standard)
  • HY-125655
    UNC-4219 TFA
    		Control
    UNC-4219 TFA is a negative control for the CBX7-H3 antagonist UNC3866 (HY-100832) and does not interact with CBX7 at high concentrations.
    UNC-4219 TFA
  • HY-101512R
    A-395 (Standard)
    		Inhibitor
    A-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.
    A-395 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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