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-161670
    NSD2-PWWP1 ligand 1
    		Inhibitor
    NSD2-PWWP1 ligand 1 (compound 34) is a small molecule ligand targeting the NSD2-PWWP1 domain (pIC50: 8.2). NSD2 is a large multidomain protein with histone writer and histone reader functions. Dysregulation of the levels of histone methyltransferase nuclear receptor binding SET domain 2 (NSD2) may lead to a variety of hematological and solid malignancies. NSD2-PWWP1 ligand 1 binds to NSD2, reducing its enzymatic activity and inhibiting tumorigenesis.
    NSD2-PWWP1 ligand 1
  • HY-156153
    CARM1 degrader-2
    		Inhibitor
    PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration.
    CARM1 degrader-2
  • HY-133567
    SET7-IN-DC21
    		Inhibitor
    SET7-IN-DC21 is a selective, potent SET7 inhibitor (IC50 = 15.93 μM; KD = 18.00 μM). SET7-IN-DC21 has good selectivity for several other epigenetic targets, such as SUV39H1, G9a, NSD1, DOT1L and MOF. SET7-IN-DC21 can be used for the researches of cancer, infection, inflammation, metabolic and cardiovascular disease, such as breast cancer.
    SET7-IN-DC21
  • HY-177400
    NSD-IN-5
    		Inhibitor
    NSD-IN-5 is a nuclear receptor-binding SET domain (NSD) inhibitor with IC50 values of 6 nM and < 1 nM against NSD1 and NSD2, respectively. NSD-IN-5 can be used in research related to multiple myeloma.
    NSD-IN-5
  • HY-163434
    PRMT5/EGFR-IN-1
    		Inhibitor
    PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors.
    PRMT5/EGFR-IN-1
  • HY-181157
    T/E PPI-IN-1
    		Inhibitor
    T/E PPI-IN-1 (Compound C87) is a TRIM28-EZH2 interaction inhibitor targeting reactive cysteines at the interface. T/E PPI-IN-1 can be used for the research of cancer.
    T/E PPI-IN-1
  • HY-161083
    PARP/EZH2-IN-2
    		Inhibitor
    PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy.
    PARP/EZH2-IN-2
  • HY-136809
    PRMT6-IN-2
    		Inhibitor
    PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.
    PRMT6-IN-2
  • HY-124699
    MMSET-IN-1
    		Inhibitor
    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET.
    MMSET-IN-1
  • HY-182366
    EED-IN-5
    		Inhibitor
    EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis.
    EED-IN-5
  • HY-168920
    NSD-IN-4
    		Inhibitor
    NSD-IN-4 (Compound A8) is a potent and an orally active NSD3 inhibitor. NSD-IN-4 induces Apoptosis in a dose-dependent manner. NSD-IN-4 exhibits significant antitumor effects against lung squamous carcinoma.
    NSD-IN-4
  • HY-112080A
    (R)-BAY-6035
    		Inhibitor
    (R)-BAY-6035 is a novel inhibitor that selectively targets the methylation of MAP3K2 by SMYD3, demonstrating nanomolar potency and specificity against kinases and other protein lysine methyltransferases.
    (R)-BAY-6035
  • HY-170831
    DS79932728
    		Inhibitor
    DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models.
    DS79932728
  • HY-168143
    YD1342
    		Inhibitor
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors..
    YD1342
  • HY-168842
    PRMT5-IN-47
    		Inhibitor
    PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity.
    PRMT5-IN-47
  • HY-181331
    PROTAC EZH2 Degrader-27
    		Inhibitor
    PROTAC EZH2 Degrader-27 is a EZH2 PROTAC inhibitor with an IC50 of 4.00 nM against EZH2. PROTAC EZH2 Degrader-27 inhibits methyltransferase activity by interacting with the SET domain of EZH2.
    PROTAC EZH2 Degrader-27
  • HY-P990434
    Anti-Histone H3 Antibody
    		Inhibitor
    The Anti-Histone H3 Antibody is a CHO-expressed humanized antibody that targets Histone H3. The Anti-Histone H3 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-Histone H3 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Histone H3 Antibody
  • HY-119164
    DC-S238
    		Inhibitor
    DC-S238 is an orally active and highly selective histone methyltransferase SET7 (SETD7) inhibitor (IC50=4.88 μM). DC-S238 is promising for research of cancer, diabetes and inflammatory diseases.
    DC-S238
  • HY-144188
    PRMT5-IN-17
    		Inhibitor
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
    PRMT5-IN-17
  • HY-161419
    EZH2-IN-18
    		Inhibitor
    EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells.
    EZH2-IN-18
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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