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-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
  • 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-W013500
    (1-Nitroethene-1,2-diyl)dibenzene
    		Inhibitor
    (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-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-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-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-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-121493
    TM2-115
    		Inhibitor 98.37%
    TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.
    TM2-115
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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