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-110158
    UNC2327
    		Inhibitor 99.70%
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
    UNC2327
  • HY-122640
    NPD13668
    		Inhibitor
    NPD13668 is an EZH2-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer.
    NPD13668
  • HY-162939
    TB22
    		Inhibitor
    TB22 is a non-nucleoside inhibitor of DOT1LR231Q, possessing anticancer activity. TB22 inhibits the malignant phenotype of lung cancer cells carrying the R231Q mutation through the MAPK/ERK signaling pathway, and can be used for lung cancer research.
    TB22
  • HY-143616
    EZH2-IN-7
    		Inhibitor
    EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259).
    EZH2-IN-7
  • HY-152775A
    RK-0133114
    		Inhibitor
    RK-0133114 is a G9a inhibitor and a R-enantiomer of RK-701 (HY-152775). RK-0133114 inhibits G9a with an IC50 value of 3.7 μM. RK-0133114 can be used for the research of sickle cell disease (SCD).
    RK-0133114
  • HY-169708
    PRMT5-IN-49
    		Inhibitor
    PRMT5-IN-49 (Compound 4b16) is an inhibitor of PRMT5.
    PRMT5-IN-49
  • HY-155818
    NSD2-IN-4
    		Inhibitor
    NSD2-IN-4 is a potent and selective NSD2-SET inhibitor. NSD2-IN-4 has the potential for NSD2-related diseases.
    NSD2-IN-4
  • HY-139823A
    PRMT5-IN-11
    		Inhibitor
    PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
    PRMT5-IN-11
  • HY-115619
    EPZ004777 formate
    		Inhibitor
    EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.
    EPZ004777 formate
  • HY-172732
    PRMT5-IN-50
    		Inhibitor
    PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice.
    PRMT5-IN-50
  • HY-115758
    PRMT1-IN-1
    		Inhibitor
    PRMT1-IN-1 is a PRMT1 inhibitor.
    PRMT1-IN-1
  • HY-139823
    PRMT5-IN-10
    		Inhibitor
    PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
    PRMT5-IN-10
  • HY-142093
    NSD3-IN-1
    		Inhibitor
    NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC50 value of 28.58 μM.
    NSD3-IN-1
  • HY-162230
    PRMT5-IN-33
    		Inhibitor
    PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity.
    PRMT5-IN-33
  • HY-178485
    SJY26
    		Inhibitor
    SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia.
    SJY26
  • HY-181849
    MS2928
    		Inhibitor
    MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma.
    MS2928
  • HY-145444
    EPZ028862
    		Inhibitor
    EPZ028862 is a selective SMYD3 inhibitor for cancer research.
    EPZ028862
  • HY-104009
    GSK2807
    		Inhibitor
    GSK2807 is a potent and selective SAM-competitive inhibitor of SMYD3, exhibiting a Ki value of 14 nM, and it may be useful for cancer treatment by preventing the methylation of MEKK2.
    GSK2807
  • HY-161869
    LSD1-IN-32
    		Inhibitor
    LSD1-IN-32 (compound 11e) is a potent LSD1 inhibitor with an IC50 value of 0.99 µM. LSD1-IN-32 inhibits RANKL-induced osteoclastogenesis, bone resorption and F-actin belt formation. LSD1-IN-32 has the potential for the research of osteoporosis.
    LSD1-IN-32
  • HY-172368
    PROTAC CARM1/IKZF3 degrader-1
    		Inhibitor
    PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
    PROTAC CARM1/IKZF3 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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