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-180553
    NSD2-IN-6
    		Inhibitor
    NSD2-IN-6 is a selective and orally active NSD2 inhibitor with IC50s of 3.8  and 274 nM for NSD2 and NSD1 respectively. NSD2-IN-6 reduces H3K36me2 levels, reverses cell plasticity by restoring the androgen receptor (AR) signaling pathway. NSD2-IN-6 reduces a shift from cluster 2 and 3 states towards the cluster 1 state in organoids. NSD2-IN-6 exerts antitumor activity by reversing tumor cell plasticity, suppressing growth, and promoting apoptosis in vivo. NSD2-IN-6 can be used for prostate cancer research.
    NSD2-IN-6
  • HY-185582
    EZH2 ligand-4
    EZH2 ligand-4 (Precursor 1) is a ligand for the target protein for PROTAC (EZH2). EZH2 ligand-4 can be used to synthesize MS8847 (HY-162250).
    EZH2 ligand-4
  • HY-161787
    G9a-IN-2
    		Inhibitor
    G9a-IN-2 (Compound 7i) is an inhibitor for histone methyltransferases G9a with IC50 of 0.024 μM. G9a-IN-2 reduces H3K9me2 levels and induces the mRNA expression of γ-globin mRNA. G9a-IN-2 shows the potential in ameliorating sickle cell disease (SCD).
    G9a-IN-2
  • HY-169400
    HDACs/EZH2-IN-1
    		Inhibitor
    HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis.
    HDACs/EZH2-IN-1
  • HY-179499
    PROTAC EZH2 Degrader-9
    		Degrader
    PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research.
    PROTAC EZH2 Degrader-9
  • HY-178378
    G9a-IN-4
    		Inhibitor
    G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer.
    G9a-IN-4
  • HY-181393
    EZH2 ligand-3
    		Ligand
    EZH2 ligand-3, a EZH2 ligand, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). EZH2 ligand-3 can be used for the synthesis of PROTAC EZH2 Degrader-35 (HY-181392).
    EZH2 ligand-3
  • HY-181327
    PROTAC EZH2 Degrader-26
    		Degrader
    PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM.
    PROTAC EZH2 Degrader-26
  • HY-156455
    SETD7-IN-1
    		Inhibitor
    SETD7-IN-1 (compound 7) is a PFI-2 (HY-18627) analogue. SETD7-IN-1 is a substrate and inhibitor of histone lysine methyltransferase SETD7, with an IC50 of 0.96 ± 0.10 µM.
    SETD7-IN-1
  • HY-145762
    YM281
    		Inhibitor
    YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma.
    YM281
  • HY-181334
    PROTAC EZH2 Degrader-39
    PROTAC EZH2 Degrader-39 (compound 18) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 61.00 nM. PROTAC EZH2 Degrader-39 functionally inhibits EZH2 methyltransferase activity.
    PROTAC EZH2 Degrader-39
  • HY-153421
    PRMT5-IN-28
    		Inhibitor
    PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape.
    PRMT5-IN-28
  • HY-118990
    Lobelane hydrochloride
    Lobelane hydrochloride is a biologically active compound that has the activity of inhibiting vesicular monoamine transporter-2 (VMAT2). Lobelane hydrochloride has a low affinity for nicotinic acetylcholine receptors (nAChR), thereby enhancing its selectivity for VMAT2. Synthetic structural changes of lobelane hydrochloride have led to some related analogs that show mild changes in affinity for VMAT2. The most potent synthetic lobelane hydrochloride obtained after structural modification has a K(i) value of 630 nM, showing significant VMAT2 selectivity. The biological activity of lobelane hydrochloride suggests that it has the potential to be used in the development of compounds to inhibit methamphetamine abuse.
    Lobelane hydrochloride
  • HY-169761
    (rac)-dWIZ-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.
    (rac)-dWIZ-1
  • HY-181309
    PROTAC EZH2 Degrader-15
    		Degrader
    PROTAC EZH2 Degrader-15 (compound 5) is an EZH2-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits EZH2 methyltransferase activity.
    PROTAC EZH2 Degrader-15
  • HY-176534
    PRMT5-IN-52
    		Inhibitor
    PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma.
    PRMT5-IN-52
  • HY-146810
    PRMT4-IN-1
    		Inhibitor
    PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC50=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability.
    PRMT4-IN-1
  • HY-101512D
    rel-A-395 hydrochloride
    		Inhibitor
    rel-A-395 hydrochloride is the relative configuration of A-395 (HY-101512) hydrochloride. A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
    rel-A-395 hydrochloride
  • HY-133031
    CSV0C018875
    		Inhibitor
    CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294.
    CSV0C018875
  • HY-179651
    NSD2-PWWP1-IN-6
    		Inhibitor
    NSD2-PWWP1-IN-6 (Compound 16) is an effective NSD2-PWWP1 inhibitor with a Kd value of 30 nM. NSD2-PWWP1-IN-6 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-6 can be used for cancer research.
    NSD2-PWWP1-IN-6
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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