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-W013500
    (1-Nitroethene-1,2-diyl)dibenzene
    		Inhibitor 99.05%
    (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.
    (1-Nitroethene-1,2-diyl)dibenzene
  • HY-122223
    EPZ030456
    		Inhibitor
    EPZ030456 is a potent and selective SMYD3 inhibitor with an IC50 of 48 nM. EPZ030456 can be used for cancer research.
    EPZ030456
  • HY-164500
    MC3629
    		Inhibitor
    MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness.
    MC3629
  • HY-B1322BR
    Amodiaquine dihydrochloride (Standard)
    		Inhibitor
    Amodiaquine (dihydrochloride) (Standard) is the analytical standard of Amodiaquine (dihydrochloride). This product is intended for research and analytical applications. Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride 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 (Standard)
  • HY-168164
    4-Methoxycinnamyl alcohol
    4-Methoxycinnamyl alcohol is an anticancer compound with cytotoxic activity against MCF-7, HeLa, and DU145 cancer cell lines with IC50 values of 14.24, 7.82, and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol showed the ability to induce cell necrosis, rather than apoptosis, after a 48-hour DNA fragmentation assay. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare.
    4-Methoxycinnamyl alcohol
  • HY-103663R
    MAK683 (Standard)
    		Inhibitor
    MAK683 (Standard) is the analytical standard of MAK683 (HY-103663). This product is intended for research and analytical applications. MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
    MAK683 (Standard)
  • HY-19546A
    (R)-BAY-598
    		Inhibitor
    (R)-BAY-598 ((R)-4) is a potent inhibitor of protein-lysine methyltransferase SMYD2, with the IC50 of 1.7 μM.
    (R)-BAY-598
  • HY-10442R
    3-Deazaneplanocin A (Standard)
    		Inhibitor
    3-Deazaneplanocin A (Standard) is the analytical standard of 3-Deazaneplanocin A (HY-10442). This product is intended for research and analytical applications. 3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.
    3-Deazaneplanocin A (Standard)
  • HY-164479
    GA001
    		Antagonist
    GA001 is a potent G9a antagonist, with an IC50 of 1.32 μM. GA001 induces autophagy and apoptosis that can be used for the breast cancer.
    GA001
  • HY-175630
    BI-9321-C10-acid
    		Ligand
    BI-9321-C10-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for NSD3 (HY-114208) and a PROTAC linker (HY-114208). BI-9321-C10-acid can be used for synthesis of PROTAC NSD3 degrader-1 (HY-155816).
    BI-9321-C10-acid
  • HY-129441R
    Metoprine (Standard)
    		Inhibitor
    Metoprine (Standard) is the analytical standard of Metoprine. This product is intended for research and analytical applications. Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
    Metoprine (Standard)
  • HY-13980R
    UNC0642 (Standard)
    		Inhibitor
    UNC0642 (Standard) is the analytical standard of UNC0642. This product is intended for research and analytical applications. UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
    UNC0642 (Standard)
  • HY-101564R
    Onametostat (Standard)
    		Inhibitor
    Onametostat (Standard) is the analytical standard of Onametostat (HY-101564). This product is intended for research and analytical applications. Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer.
    Onametostat (Standard)
  • HY-110137R
    Furamidine dihydrochloride (Standard)
    		Inhibitor
    Furamidine (dihydrochloride) (Standard) is the analytical standard of Furamidine (dihydrochloride). This product is intended for research and analytical applications. Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
    Furamidine dihydrochloride (Standard)
  • HY-107777AR
    LLY-284 (Standard)
    		Control
    LLY-284 (Standard) is the analytical standard of LLY-284 (HY-107777A). This product is intended for research and analytical applications. LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.
    LLY-284 (Standard)
  • HY-169113
    EPZ032597
    		Inhibitor
    EPZ032597 is a selective and noncompetitive SMYD2 inhibitor with an IC50 value of 16 nM. EPZ032597 is promising for research of pancreatic ductal adenocarcinoma.
    EPZ032597
  • HY-B1377
    Acedapsone
    Acedapsone is a compound with antimalarial and antimicrobial activities. Acedapsone is mainly used as a long-acting leprosy inhibitor.
    Acedapsone
  • HY-101938R
    Sinefungin (Standard)
    		Inhibitor
    Sinefungin (Standard) is the analytical standard of Sinefungin (HY-101938). This product is intended for research and analytical applications. Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation.
    Sinefungin (Standard)
  • HY-P10425
    T2857W
    		Inhibitor
    T2857W is a mutant peptide that has inhibitory effect on KIX-MLL interaction (IC50=5.67 μM). T2857W can be used for protein-protein interaction (PPI) and for the study of diseases related to KIX-MLL interaction, such as leukemia, cancer, etc.
    T2857W
  • HY-B1322AR
    Amodiaquine (Standard)
    		Inhibitor
    Amodiaquine (Standard) is the analytical standard of Amodiaquine. This product is intended for research and analytical applications. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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