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-150510
    MS8511
    		Inhibitor
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
    MS8511
  • HY-122936
    Tanshindiol C
    		Inhibitor 98.47%
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
    Tanshindiol C
  • HY-162783
    AZ-PRMT5i-1
    		Inhibitor
    AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective PRMT5 inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers.
    AZ-PRMT5i-1
  • HY-15214
    CARM1-IN-3
    		Inhibitor 98.90%
    CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
    CARM1-IN-3
  • HY-148669B
    (S)-Bleximenib oxalate
    		Control 98.37%
    (S)-Bleximenib (oxalate) is a S-Enantiomer of Bleximenib oxalate (HY-148669A). Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia.
    (S)-Bleximenib oxalate
  • HY-P10948A
    CS-VIP 8 hydrochloride
    		Inhibitor
    CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia.
    CS-VIP 8 hydrochloride
  • HY-161313
    DYB-03
    		Inhibitor 99.49%
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2- and GSK126-resistant of A549 and H460 cells.
    DYB-03
  • HY-161796A
    UNC8732 TFA
    		Inhibitor 99.07%
    UNC8732 (TFA) is a NSD2 inhibitor and degrader.
    UNC8732 TFA
  • 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-164456
    AMI-408
    		Inhibitor
    AMI-408 is a PRMT1 inhibitor. AMI-408 can reduce H4R3me2as level in MLL-GAS7 leukemia cells.
    AMI-408
  • HY-161017
    WDR91-IN-1
    		98.90%
    WDR91-IN-1 (Compd 1) is a first-in-class small-molecule ligand for WDR91, with a KD of 6 μM.
    WDR91-IN-1
  • HY-149726
    EZH2-IN-17
    		Inhibitor 98.08%
    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-178065
    PROTAC G9a/GLP degrader 1
    		Degrader 98.22%
    PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)).
    PROTAC G9a/GLP degrader 1
  • HY-126327
    UNC4976
    		Antagonist
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
    UNC4976
  • HY-160865
    PRMT5-IN-35
    		Inhibitor 99.63%
    PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM. PRMT5-IN-35 can be used in cancer research.
    PRMT5-IN-35
  • HY-B1322R
    Amodiaquine dihydrochloride dihydrate (Standard)
    		Inhibitor
    Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine dihydrochloride dihydrate (Standard)
  • HY-16986A
    EPZ011989 trifluoroacetate
    		Inhibitor 98.71%
    EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EPZ011989 trifluoroacetate
  • HY-144881
    (S)-HH2853
    		Inhibitor
    (S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases.
    (S)-HH2853
  • 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-126256
    PRMT5-IN-1
    		Inhibitor
    PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
    PRMT5-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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