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-134086
    NSD-IN-2
    		Inhibitor
    NSD-IN-2 (compound 151) is a potent and irreversible NSD1 inhibitor. NSD-IN-2 can be used in research of cancer.
    NSD-IN-2
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
    		Degrader 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma.
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
  • HY-122182
    OTS193320
    		Inhibitor 98.64%
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX.
    OTS193320
  • HY-124131
    DS-437
    		Inhibitor 99.22%
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
    DS-437
  • HY-145103
    UNC6934
    		Chemical 99.15%
    UNC6934, a chemical probe targeting the PWWP domain, alters NSD2 nucleolar localization.
    UNC6934
  • HY-139400A
    Pociredir hydrochloride
    		Inhibitor 99.89%
    Pociredir (FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir hydrochloride can induce HbF protein expression in cell and murine models. Pociredir hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.
    Pociredir hydrochloride
  • HY-141430
    AS-85
    		Inhibitor 98.96%
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 μM.
    AS-85
  • HY-117421A
    CM-579 trihydrochloride
    		Inhibitor
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
    CM-579 trihydrochloride
  • HY-12759
    CARM1-IN-1
    		Inhibitor
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.
    CARM1-IN-1
  • HY-112080
    BAY-6035
    		Inhibitor 99.82%
    BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM.
    BAY-6035
  • HY-15227A
    EPZ004777 hydrochloride
    		Inhibitor 99.46%
    EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
    EPZ004777 hydrochloride
  • HY-130615
    PROTAC EED degrader-2
    		Inhibitor 99.90%
    PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.
    PROTAC EED degrader-2
  • HY-155814
    EML734
    		Inhibitor 99.48%
    EML734 is a potent and selective PRMT7/9 inhibitor with IC50 values of 315 nM and 0.89 μM, respectively.
    EML734
  • HY-155170
    MTDH-SND1 blocker 1
    		Inhibitor 99.33%
    MTDH-SND1 blocker 1 (compound C26-A6) is an inhibitor of the MTDH-SND1 protein. MTDH-SND1 blocker 1 inhibits cancer metastasis.
    MTDH-SND1 blocker 1
  • HY-148458
    EZH2-IN-14
    		Inhibitor 99.02%
    EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1.
    EZH2-IN-14
  • HY-100025A
    HLCL-61 hydrochloride
    		Inhibitor 99.87%
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
    HLCL-61 hydrochloride
  • HY-128717
    GSK3368715
    		Inhibitor 99.19%
    GSK3368715 (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 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
    GSK3368715
  • HY-100360
    MS049
    		Inhibitor ≥98.0%
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
    MS049
  • HY-111778
    EHMT2-IN-1
    		Inhibitor 99.85%
    EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
    EHMT2-IN-1
  • HY-15226A
    AZ505 ditrifluoroacetate
    		Inhibitor 99.91%
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
    AZ505 ditrifluoroacetate
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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