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-164497
    NSC 641396
    		Inhibitor
    NSC 641396 is a ribonucleotide reductase (RNR) inhibitor with an IC50 value of 1.2 μM. NSC 641396 is also a protein arginine N-methyltransferase 9 (PRMT9) inhibitor. NSC 641396 has antitumor activity.
    NSC 641396
  • HY-182892
    MC4491
    		Inhibitor
    MC4491 is a selective LSD1/PRMT5 inhibitor, with an IC50 of 0.152 μM against the LSD1/CoREST complex and an IC50 of 0.043 μM against the PRMT5/MEP50 complex. MC4491 induces transcriptomic changes and splicing alterations in AML cells. MC4491 is applicable for the research of acute myeloid leukemia.
    MC4491
  • HY-169958
    EZH2-IN-22
    		Inhibitor
    EZH2-IN-22 (example 92) is a potent EZH2 inhibitor with IC50 values of <0.00051, <0.00051, 0.00052 µM for EZH2 (Y641N), EZH2 (Y641F), EZH2 (wt), respectively. EZH2-IN-22 shows antiproliferation activity.
    EZH2-IN-22
  • HY-144189
    PRMT5-IN-18
    		Inhibitor
    PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5， such as cancer.
    PRMT5-IN-18
  • HY-178110
    HDAC6-IN-65
    		Inducer
    HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma.
    HDAC6-IN-65
  • HY-174983
    PRMT5-MTA-IN-6
    		Inhibitor
    PRMT5-MTA-IN-6 (Compound 31) is a selective MTA-cooperative PRMT5 inhibitor. PRMT5-MTA-IN-6 exhibits potent inhibitory activity against PRMT5・MTA (IC50: 6.6 nM). PRMT5-MTA-IN-6 selectively inhibits the growth of MTAP-deleted HCT-116 cells (IC50: 319 nM). PRMT5-MTA-IN-6 can be used in the research of MTAP-deleted tumors.
    PRMT5-MTA-IN-6
  • HY-150680
    SARS-CoV-2 nsp14-IN-1
    		Antagonist
    SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.
    SARS-CoV-2 nsp14-IN-1
  • 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-181521
    RAPRMT5
    		Degrader
    RAPRMT5 is a PRMT5 CAP-TAC (proteinase complex-targeted chimeric agent) degrader. RAPRMT5 can induce PRMT5 to undergo proteasome-dependent, ubiquitin-independent degradation. RAPRMT5 can be used in the research of various cancers.
    RAPRMT5
  • 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-183354
    HLC40
    		Inhibitor
    HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model.
    HLC40
  • HY-P2252
    H3K27(Me) (15-34)
    H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me).
    H3K27(Me) (15-34)
  • 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-172733S
    PRMT5-MTA-IN-3-d3
    		Inhibitor
    PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer.
    PRMT5-MTA-IN-3-d<sub>3</sub>
  • 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-183653
    AK442
    		Inhibitor
    AK442 is a selective PRMT4 (CARM1) inhibitor with an IC50 of 2.6 nM against human targets. AK442 is applicable to breast cancer-related research.
    AK442
  • 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-173423
    DOT1L ligand-1
    		Ligand
    DOT1L ligand-1 is a DOT1L ligand. DOT1L ligand-1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as MS2133 (HY-173422).
    DOT1L ligand-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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