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-100832A
    UNC3866 TFA
    		Inhibitor
    UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
    UNC3866 TFA
  • HY-158158
    CARM1-IN-5
    		Inhibitor
    CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines.
    CARM1-IN-5
  • HY-162989
    PRMT5-MTA-IN-2
    		Inhibitor
    PRMT5-MTA-IN-2 (compund 1) is a MTA co-inhibitor of PRMT5 with IC50 less than 1.5 nM.
    PRMT5-MTA-IN-2
  • HY-156096
    HDAC3-IN-2
    		Modulator
    HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels.
    HDAC3-IN-2
  • HY-168263
    PRMT5-IN-45
    		Inhibitor
    PRMT5-IN-45 (compound 36) is a potent and selective PRMT5 inhibitor with an IC50 of 3 nM. PRMT5-IN-45 potently reduces the level of symmetric dimethylarginines (sDMA) and inhibits the proliferation of MOLM-13 cell lines by inducing apoptosis and cell cycle arrest.
    PRMT5-IN-45
  • HY-153422
    PRMT5-IN-29
    		Inhibitor 98.01%
    PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research.
    PRMT5-IN-29
  • HY-122746
    E67-2
    		Inhibitor
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.
    E67-2
  • HY-163592
    PRMT5-IN-43
    		Inhibitor
    PRMT5-IN-43 (compound 4A) is a PRMT5 inhibitor. PRMT5-IN-43 can be used in cancer research.
    PRMT5-IN-43
  • HY-170674A
    ND-L11B TFA
    		Degrader
    ND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 %.
    ND-L11B TFA
  • HY-159732
    PRMT3-IN-4
    		Inhibitor
    PRMT3-IN-4 (intermediate 15) is a protein arginine methyltransferase 3 (PRMT3) inhibitor. PRMT3-IN-4 is an active control for HY-19715. PRMT3-IN-4 can be used to synthesize PROTACs targeting PRMT3. PRMT3-IN-4 can be used in leukemia-related research.
    PRMT3-IN-4
  • HY-P10570
    [Nle20] H4 peptide (16−23)
    		Inhibitor
    [Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 (Kd=0.14 μM), which inhibits SETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy.
    [Nle20] H4 peptide (16−23)
  • HY-163593
    PRMT5-IN-44
    		Inhibitor
    PRMT5-IN-44 (compound 12) is a PRMT5 inhibitor. PRMT5-IN-44 can be used in cancer research.
    PRMT5-IN-44
  • HY-163818
    WIZ degrader 2
    		Degrader
    WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders.
    WIZ degrader 2
  • HY-144096
    EZH2-IN-11
    EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17).
    EZH2-IN-11
  • HY-B1322AS1
    Amodiaquine-d10 hydrochloride
    		Inhibitor
    Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). 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-d<sub>10</sub> hydrochloride
  • HY-146285
    LSD1-IN-20
    		Inhibitor
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively.
    LSD1-IN-20
  • HY-162601
    D-01
    		Inhibitor
    D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer.
    D-01
  • HY-132937
    PRMT5-IN-9
    		Inhibitor
    PRMT5-IN-9 is a novel PRMT5 inhibitor for researching cancer, with an IC50 of 0.01 μM.
    PRMT5-IN-9
  • HY-161334
    CARM1-IN-4
    		Inhibitor
    CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity.
    CARM1-IN-4
  • HY-133031A
    CSV0C018875 hydrochloride
    		Inhibitor
    CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization.
    CSV0C018875 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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