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-154854
    BBDDL2059
    		Inhibitor
    BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research.
    BBDDL2059
  • HY-160029
    PRMT5-IN-32
    		Inhibitor
    PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM.
    PRMT5-IN-32
  • HY-122991
    Prospasmine hydrochloride
    Prospasmine hydrochloride is an anticholinergic drug that has the activity of inhibiting glandular secretions and relaxing smooth muscles. Prospasmine hydrochloride is mainly used to inhibit certain types of gastrointestinal disorders. Prospasmine hydrochloride helps relieve pain caused by smooth muscle spasms. Prospasmine hydrochloride is also used as an anesthetic adjuvant in some cases.
    Prospasmine hydrochloride
  • HY-150510A
    MS8511 hydrochloride
    		Inhibitor
    MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
    MS8511 hydrochloride
  • HY-155154A
    PRMT4-IN-3
    		Inhibitor
    PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50: 37 nM) and PRMT4 (IC50: 253 nM).
    PRMT4-IN-3
  • HY-163590
    PRMT5-IN-41
    		Inhibitor
    PRMT5-IN-41 (compound 130) is a potent and orally active PRMT5 inhibitor. PRMT5-IN-41 inhibits hERG ion channel with IC50 value of 1.36 µM.
    PRMT5-IN-41
  • HY-162003
    DCPT1061
    		Inhibitor 99.81%
    DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 has antitumor effect.
    DCPT1061
  • HY-162749
    G9D-4
    		Degrader
    G9D-4 is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)).
    G9D-4
  • HY-158143
    PRMT5-IN-34
    		Inhibitor
    PRMT5-IN-34 (Compound C) is an inhibitor of MTA-cooperative Protein arginine methyltransferase 5 (PRMT5/MAT).
    PRMT5-IN-34
  • HY-P990574
    Derlotuximab
    		Inhibitor
    Derlotuximab is a CHO-expressed, scFv-Fc (huIgG1) type chimeric antibody that targets Histone H1. The predicted molecular weight (MW) of Derlotuximab is 145.1 kDa. The isotype control for Derlotuximab can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Derlotuximab
  • HY-139150
    EZH2-IN-4
    		Inhibitor
    EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.
    EZH2-IN-4
  • HY-163288
    EZH2/HSP90-IN-29
    		Inhibitor
    EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
    EZH2/HSP90-IN-29
  • HY-12707A
    Piribedil dihydrochloride
    		Inhibitor
    Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil dihydrochloride
  • HY-122595
    EZH2-IN-1
    		Inhibitor
    EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research.
    EZH2-IN-1
  • HY-163589
    PRMT5-IN-40
    		Inhibitor
    PRMT5-IN-40 (compound 104) is a potent inhibitor of PRMT5.
    PRMT5-IN-40
  • HY-110137A
    Furamidine
    		Inhibitor
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
    Furamidine
  • HY-149463
    EZH2-IN-16
    		Inhibitor
    EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC50 of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI50 of 0.2 μM.
    EZH2-IN-16
  • HY-P5922
    PTD2
    		Inhibitor
    PTD2 (Ac-Gly-Val-Nle-Arg-Ile-NH2) is a potent, selective inhibitor of WHSC1. PTD2 exhibits micromolar affinity towards WHSC1.
    PTD2
  • HY-P2266
    SAH-EZH2
    		Inhibitor
    SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27.
    SAH-EZH2
  • HY-168083
    Dot1L-IN-9
    		Inhibitor
    Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor (IC50: 125 nM). Dot1L-IN-9 reduces H3K79 dimethylation. Dot1L-IN-9 can be used for anti-leukemia research.
    Dot1L-IN-9
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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