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-145602
    Tulmimetostat
    		Inhibitor 99.79%
    Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.
    Tulmimetostat
  • 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-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-125292
    NV03
    		Antagonist 98.82%
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
    NV03
  • 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-136977
    EEDi-5285
    		Inhibitor 99.98%
    EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
    EEDi-5285
  • HY-130815A
    MAK683-CH2CH2COOH hydrochloride
    		Inhibitor 98.03%
    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615).
    MAK683-CH2CH2COOH hydrochloride
  • HY-148674
    PRMT5-IN-25
    		Inhibitor 99.94%
    PRMT5-IN-25 (compound 503) is a potent PRMT5 inhibitor with an Ki value of 0.06 nM. PRMT5-IN-25 shows antiproliferative.
    PRMT5-IN-25
  • HY-130614
    PROTAC EED degrader-1
    		Inhibitor 98.27%
    PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
    PROTAC EED degrader-1
  • 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-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-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-151379
    EM127
    		Inhibitor 98.37%
    EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours.
    EM127
  • HY-122096
    DCLX069
    		Inhibitor 98.03%
    DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects.
    DCLX069
  • HY-114340
    LEM-14
    		Inhibitor 98.06%
    LEM-14 is a potent NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has the potential for the research of multiple myeloma.
    LEM-14
  • HY-132922
    EEDi-5273
    		Inhibitor 99.09%
    EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC50 = 0.2 nM) capable of achieving complete and persistent tumor regression.
    EEDi-5273
  • 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-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-15226A
    AZ505 ditrifluoroacetate
    		Inhibitor 99.91%
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
    AZ505 ditrifluoroacetate
  • HY-124131
    DS-437
    		Inhibitor 98.00%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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