1. Signaling Pathways
  2. Epigenetics
  3. DNA Methyltransferase

DNA Methyltransferase

DNMTs; DNA MTases

DNA methyltransferases (DNMTs) are a family of “writer” enzymes responsible for DNA methylation that is the addition of a methyl group to the carbon atom number five (C5) of cytosine. Mammalians encode five DNMTs: DNMT1, DNMT2, DNMT3A-DNMT3B (de novo methyltransferases), and DNMTL. DNMT1, DNMT3A, and DNMT3B are the three active enzymes that maintain DNA methylation. DNMT3L has no catalytic activity and functions as a regulator of DNMT3A and DNMT3B, whereas DNMT2 acts as a tRNA transferase rather than a DNA methyltransferase.

DNA methylation is a vital modification process in the control of genetic information, which contributes to the epigenetics by regulating gene expression without changing the DNA sequence. In prokaryotes, DNA methylation is essential for transcription, the direction of post-replicative mismatch repair, the regulation of DNA replication, cell-cycle control, bacterial virulence, and differentiating self and non-self DNA. In mammalians, DNA methylation is crucial in many key physiological processes, including the inactivation of the X-chromosome, imprinting, and the silencing of germline-specific genes and repetitive elements.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15449A
    (S)-Kaempferide
    Inhibitor
    (S)-Kaempferide (ZINC167686681) is a DNA methyltransferase (DNMT) inhibitor. (S)-Kaempferide can be used in tumor research.
    (S)-Kaempferide
  • HY-E70209
    EcoRI Methyltransferase
    EcoRI Methyltransferase is a bacterial sequence-specific S-adenosyl-L-methionine-dependent DNA methyltransferase. EcoRI Methyltransferase relies on a complex conformational mechanism to achieve its remarkable specificity, including DNA bending, base flipping and intercalation into the DNA.
    EcoRI Methyltransferase
  • HY-A0084AR
    Procainamide (Standard)
    Inhibitor
    Procainamide (Standard) is the analytical standard of Procainamide. This product is intended for research and analytical applications. Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research.
    Procainamide (Standard)
  • HY-170523
    RU-0415529
    Inhibitor
    RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models.
    RU-0415529
  • HY-170524
    TDI-015051
    Inhibitor
    TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC50=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC50=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC50s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models.
    TDI-015051
  • HY-154867
    DNMT2-IN-1
    Inhibitor
    DNMT2-IN-1 (compound 80) is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research.
    DNMT2-IN-1
  • HY-151446
    ZIKV-IN-3
    Inhibitor
    ZIKV-IN-3 (compound 5a), an andrographolide derivatives, is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 18.34 μM. ZIKV-IN-3 inhibits ZIKV replication and infection. ZIKV-IN-3 can be used in research of Zika virus (ZIKV).
    ZIKV-IN-3
  • HY-150025
    (4aS,8aR)-NPD-001
    Inhibitor
    (4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882.
    (4aS,8aR)-NPD-001
  • HY-E70204
    AluI Methyltransferase
    AluI Methyltransferase (AluI) is a methyltransferase used as the interference enzymes to investigate the selectivity.
    AluI Methyltransferase
  • HY-E70206
    CpG Methyltransferase
    CpG Methyltransferase is a DNA methyltransferase. CpG Methyltransferase can methylate the C5 position on the base moiety of all cytosine nucleotides contained in unmethylated or hemimethylated double stranded DNA in a 5’-CpG-3’ context.
    CpG Methyltransferase
  • HY-168636
    p53 Activator 13
    Inhibitor
    p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNA damage response via p53 activation. p53 Activator 13 can be utilized in cancer research.
    p53 Activator 13
  • HY-112551
    2′,3′,5′-Triacetyl-5-azacytidine
    2′,3′,5′-Triacetyl-5-azacytidine is an orally active proagent of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase.
    2′,3′,5′-Triacetyl-5-azacytidine
  • HY-151445
    ZIKV-IN-2
    Inhibitor
    ZIKV-IN-2 (compound 3a) is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 38.86 μM. ZIKV-IN-2 inhibits ZIKV replication and infection. ZIKV-IN-2 can be used in research of Zika virus (ZIKV).
    ZIKV-IN-2
  • HY-133030
    DNMT-IN-1
    Inhibitor
    DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active.
    DNMT-IN-1
  • HY-126426
    CBHcy
    Inhibitor
    CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model.
    CBHcy
  • HY-106689A
    Dihydro-5-azacytidine acetate
    Inhibitor
    Dihydro-5-azacytidine acetate (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine acetate has an antitumor activity.
    Dihydro-5-azacytidine acetate
  • HY-E70211
    HaeIII Methyltransferase
    HaeIII Methyltransferase (HaeIII) is a Methyltransferase which can bind covalently to DNA.
    HaeIII Methyltransferase
  • HY-P10407
    BM30
    Inhibitor
    BM30 is a selective peptidomimetic NTMT1 and NTMT2 inhibitor (IC50: 0.89 μM for NTMT1).
    BM30
  • HY-145950
    2′-Deoxy-5-nitrocytidine
    Inhibitor
    2′-Deoxy-5-nitrocytidine is a DNA Methyltransferase inhibitor extracted from patent CN108498529A. 2′-Deoxy-5-nitrocytidine can be used for the research of cancer.
    2′-Deoxy-5-nitrocytidine
  • HY-106689
    Dihydro-5-azacytidine
    Inhibitor
    Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity.
    Dihydro-5-azacytidine
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