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-146724
    Dot1L-IN-7
    		Inhibitor
    Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells.
    Dot1L-IN-7
  • HY-164144
    EPZ033294
    		Inhibitor
    EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T.
    EPZ033294
  • HY-P3822
    PRMT5-IN-23
    		Inhibitor
    PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) 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-23
  • HY-163586
    PRMT5-IN-37
    		Inhibitor
    PRMT5-IN-37 (compound 29) is an orally active PRMT5 inhibitor and can be used for study of cancer.
    PRMT5-IN-37
  • HY-110196
    (S)-PFI-2 hydrochloride
    		Inhibitor
    (S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2.
    (S)-PFI-2 hydrochloride
  • HY-110158
    UNC2327
    		Inhibitor 99.70%
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
    UNC2327
  • HY-116971
    DCG066
    		Inhibitor
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562.
    DCG066
  • 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-10427
    WAY-260022
    WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction.
    WAY-260022
  • 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-164456
    AMI-408
    		Inhibitor
    AMI-408 is a PRMT1 inhibitor. AMI-408 can reduce H4R3me2as level in MLL-GAS7 leukemia cells.
    AMI-408
  • HY-126300
    SGC6870
    		Inhibitor
    SGC6870 is a potent, selective and cytoactive allosteric inhibitor of PRMT6 with IC50 of 77 nM.
    SGC6870
  • 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-155817
    UNC7096
    		Chemical
    UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions.
    UNC7096
  • HY-138886
    RL5a
    		Inhibitor
    RL5a (compund C23) is a SETD8 inhibitor.
    RL5a
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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