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-142095
    NSD3-IN-3
    		Inhibitor
    NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460.
    NSD3-IN-3
  • HY-162230
    PRMT5-IN-33
    		Inhibitor
    PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity.
    PRMT5-IN-33
  • HY-117542
    D595
    D595 is a phenylethylamine calcium channel blocker with potent negative inotropic activity. D595 has shown significant efficacy in its corresponding pharmacological studies, especially in inhibiting the uptake of monoamine neurotransmitters. D595 has high affinity in binding to the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). Structural adjustments of D595, especially changes in the hydroxyl stereochemistry, significantly affect its interaction with the transporters, showing a specific preference for stereoisomers.
    D595
  • HY-19554
    MM-401
    		Inhibitor
    MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia.
    MM-401
  • HY-145444
    EPZ028862
    		Inhibitor
    EPZ028862 is a selective SMYD3 inhibitor for cancer research.
    EPZ028862
  • HY-104009
    GSK2807
    		Inhibitor
    GSK2807 is a potent and selective SAM-competitive inhibitor of SMYD3, exhibiting a Ki value of 14 nM, and it may be useful for cancer treatment by preventing the methylation of MEKK2.
    GSK2807
  • HY-161869
    LSD1-IN-32
    		Inhibitor
    LSD1-IN-32 (compound 11e) is a potent LSD1 inhibitor with an IC50 value of 0.99 µM. LSD1-IN-32 inhibits RANKL-induced osteoclastogenesis, bone resorption and F-actin belt formation. LSD1-IN-32 has the potential for the research of osteoporosis.
    LSD1-IN-32
  • HY-150081
    PRMT5-IN-21
    		Inhibitor
    PRMT5-IN-21 (compound 1) is a potent cyclonucleoside PRMT5 inhibitor.
    PRMT5-IN-21
  • HY-163591
    PRMT5-IN-36-d3
    		Inhibitor
    PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research.
    PRMT5-IN-36-d<sub>3</sub>
  • HY-163741
    EZH2-IN-19
    		Inhibitor
    EZH2-IN-19 (conpound N40) is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) WT, with the IC50 of 0.32 nM. EZH2-IN-19 plays an important role in cancer research.
    EZH2-IN-19
  • HY-111589
    EPZ-4777
    		Inhibitor
    EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research.
    EPZ-4777
  • HY-145813
    MU1656
    		Inhibitor
    MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L, with an IC50 of 2 nM. MU1656 can be used for the research of hematological malignancies.
    MU1656
  • HY-144330
    TDI-6118
    		Inhibitor
    TDI-6118 (Compound 5) is a potent inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies.
    TDI-6118
  • HY-100565A
    SGC2085 hydrochloride
    		Inhibitor
    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
    SGC2085 hydrochloride
  • HY-142094
    NSD3-IN-2
    		Inhibitor
    NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity.
    NSD3-IN-2
  • HY-44062
    G9a-IN-1
    		Inhibitor 98.12%
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
    G9a-IN-1
  • 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-145452
    5-Octyl-α-ketoglutarate
    5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
    5-Octyl-α-ketoglutarate
  • HY-163774
    WDR5-MYC-IN-1
    		Inhibitor
    WDR5-MYC-IN-1 (compound 4o) is a potent WDR5-MYC interaction inhibitor with a Ki value of 1.0 µM. WDR5-MYC-IN-1 shows antiproliferative activity.
    WDR5-MYC-IN-1
  • HY-158157
    ZL-28-6
    		Inhibitor
    ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research.
    ZL-28-6
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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