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-149726
    EZH2-IN-17
    		Inhibitor
    EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively).
    EZH2-IN-17
  • HY-144882
    (R)-HH2853
    		Inhibitor
    (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201).
    (R)-HH2853
  • HY-12335A
    UNC0379 TFA
    		Inhibitor 99.91%
    UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
    UNC0379 TFA
  • HY-18627
    PFI-2
    		Inhibitor
    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
    PFI-2
  • HY-103663A
    MAK683 hydrochloride
    		Inhibitor
    MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
    MAK683 hydrochloride
  • HY-142211
    PRMT5-IN-15
    		Inhibitor
    PRMT5-IN-15 is a PRMT5 inhibitor with an IC50 value of 0.84 nM.
    PRMT5-IN-15
  • HY-100855
    DC_C66
    		Inhibitor
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5.
    DC_C66
  • HY-10587A
    BIX-01294 hydrochloride hydrate
    		Inhibitor
    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.
    BIX-01294 hydrochloride hydrate
  • HY-134899
    CPI-1328
    		Inhibitor
    CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
    CPI-1328
  • HY-19615A
    MS023 trihydrochloride
    		Inhibitor
    MS023 trihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
    MS023 trihydrochloride
  • HY-100360A
    MS049 dihydrochloride
    		Inhibitor
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells.
    MS049 dihydrochloride
  • HY-19563
    A-893
    		Inhibitor
    A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
    A-893
  • HY-101520
    Dot1L-IN-1
    		Inhibitor
    Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively.
    Dot1L-IN-1
  • HY-141876
    PRMT5-IN-14
    		Inhibitor
    PRMT5-IN-14 is a PRMT5 inhibitor to research cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
    PRMT5-IN-14
  • HY-141429C
    AS-99
    		Inhibitor
    AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
    AS-99
  • HY-128717B
    GSK3368715 trihydrochloride
    		Inhibitor
    GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
    GSK3368715 trihydrochloride
  • HY-135129
    Dot1L-IN-6
    		Inhibitor
    Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.19 nM.
    Dot1L-IN-6
  • HY-103682A
    PF-06726304 acetate
    		Inhibitor
    PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity.
    PF-06726304 acetate
  • HY-156615
    Igermetostat
    		Inhibitor
    Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro.
    Igermetostat
  • HY-141874
    PRMT5-IN-12
    		Inhibitor
    PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5.
    PRMT5-IN-12
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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