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-149289
    DNMT-IN-3
    Inhibitor
    DNMT-IN-3 is an DNA Methyltransferase (DNMT) inhibitor, and plays an antimalarial role with IC50 of 60 nM against Plasmodium falciparum (Plasmodium). DNMT-IN-3 can be used for malaria related research.
    DNMT-IN-3
  • HY-150680
    SARS-CoV-2 nsp14-IN-1
    Antagonist
    SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.
    SARS-CoV-2 nsp14-IN-1
  • HY-19826
    Isofistularin-3
    Inhibitor
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
    Isofistularin-3
  • HY-158165
    DNMT3A-IN-3
    Inhibitor
    DNMT3A-IN-3 is an allosteric DNA methyltransferase 3A (DNMT3A) inhibitor. DNMT3A-IN-3 binds and disrupt protein-protein interactions (PPIs) at the DNMT3A tetramer interface.
    DNMT3A-IN-3
  • HY-N12612
    CNP0296775
    Inhibitor
    CNP0296775 is an inhibitor of dengue virus methyltransferase (DENV MTase) that has the potential to disrupt the viral replication process.
    CNP0296775
  • HY-A0004R
    Decitabine (Standard)
    Inhibitor
    Decitabine (Standard) is the analytical standard of Decitabine. This product is intended for research and analytical applications. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
    Decitabine (Standard)
  • HY-163535
    J208
    Inhibitor
    J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs).
    J208
  • 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-10586R
    5-Azacytidine (Standard)
    Inhibitor
    5-Azacytidine (Standard) is the analytical standard of 5-Azacytidine. This product is intended for research and analytical applications. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
    5-Azacytidine (Standard)
  • HY-158164
    DNMT3A-IN-2
    Inhibitor
    DNMT3A-IN-2 (compound 1a) is a hydrophthalazinone-based inhibitor of DNA methyltransferase 3A (DNMT3A) (IC50: 14 μM) against S-adenosylmethionine (SAM) has a Ki of 9.16-18.85 μM..
    DNMT3A-IN-2
  • HY-158075
    DNMT/HDAC-IN-1
    Inhibitor
    DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.
    DNMT/HDAC-IN-1
  • HY-E70205
    BamHI Methyltransferase
    BamHI Methyltransferase is a DNA methyltransferase which modifies the underlined cytosine (GGATCC).
    BamHI Methyltransferase
  • 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-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-13765R
    6-Thioguanine (Standard)
    Inhibitor
    6-Thioguanine (Standard) is the analytical standard of 6-Thioguanine. This product is intended for research and analytical applications. 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
    6-Thioguanine (Standard)
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