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-158157
    ZL-28-6
    		Inhibitor
    ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research.
    ZL-28-6
  • HY-B1322R
    Amodiaquine (dihydrochloride dihydrate) (Standard)
    		Inhibitor
    Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine (dihydrochloride dihydrate) (Standard)
  • HY-118715
    Setin-1
    		Inhibitor
    Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a.
    Setin-1
  • HY-103641C
    Octyl-α-hydroxyglutarate
    		Agonist
    Octyl-α-hydroxyglutarate (octyl-2-HG) increases histone methylation and enhances viability of LMP1-negative NPC cells.
    Octyl-α-hydroxyglutarate
  • HY-117927
    EPZ0025654
    		Inhibitor
    EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM.
    EPZ0025654
  • HY-113846A
    CMP-5 dihydrochloride
    		Inhibitor
    CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5 dihydrochloride
  • HY-157251A
    UNC8153
    		Inhibitor
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2.
    UNC8153
  • HY-12707B
    Piribedil maleate
    		Inhibitor
    Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil maleate
  • HY-169761
    WIZ-IN-1
    		Degrader
    WIZ-IN-1 (Example 2) is a Wiz inhibitor (DC50: 0.36 μM). WIZ-IN-1 can be used for research of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
    WIZ-IN-1
  • HY-B1226
    Diperodon hydrochloride
    		Inhibitor 98.36%
    Diperodon hydrochloride exerts its effect by being broken down by serum degradoses.
    Diperodon hydrochloride
  • HY-111085
    CPI-905
    		Inhibitor
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor.
    CPI-905
  • HY-116605
    GSK926
    		Inhibitor
    GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research.
    GSK926
  • HY-100235A
    GSK591 hydrochloride
    		Inhibitor
    GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
    GSK591 hydrochloride
  • HY-122115
    DCE_42
    		Inhibitor
    DCE_42 is a potent EZH2 inhibitor with an IC50 value of 22.6 µM. DCE_42 inhibits cell proliferation and has the potential for the research of lymphoma.
    DCE_42
  • 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-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-157659
    WDR5-MLL1 antagonist 1
    		Antagonist
    WDR5-MLL1 antagonist 1 (compound 47) is a compound optimized through protein crystal structure guidance. It has stronger antagonistic activity against WDR5-MLL interaction with a dissociation constant (Kd) of 0.3μM.
    WDR5-MLL1 antagonist 1
  • 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. It 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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