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-131991
    Benzyl selenocyanate
    Inhibitor 99.84%
    Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM.
    Benzyl selenocyanate
  • HY-139015
    5-Aza-4'-thio-2'-deoxycytidine
    Inhibitor 99.09%
    5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects.
    5-Aza-4'-thio-2'-deoxycytidine
  • HY-158075
    DNMT/HDAC-IN-1
    Inhibitor 99.87%
    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-13057
    O6BTG-octylglucoside
    Inhibitor
    O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
    O6BTG-octylglucoside
  • HY-135146A
    (Rac)-GSK-3484862
    Control 99.43%
    (Rac)-GSK-3484862 is the isomer of GSK-3484862 (HY-135146), and can be used as an experimental control. GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
    (Rac)-GSK-3484862
  • HY-119390
    AA-CW236
    Inhibitor 99.86%
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification.
    AA-CW236
  • 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-133021
    Arazine
    ≥98.0%
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
    Arazine
  • 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)
  • HY-13542
    Guadecitabine
    Inhibitor 98.0%
    Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
    Guadecitabine
  • HY-111644
    6-Methyl-5-azacytidine
    Inhibitor
    6-Methyl-5-azacytidine is a potent DNMT inhibitor.
    6-Methyl-5-azacytidine
  • HY-117421
    CM-579
    Inhibitor
    CM-579 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
  • HY-139664B
    (S)-GSK-3685032
    Inhibitor 98.82%
    (S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
    (S)-GSK-3685032
  • HY-B0106R
    Levetiracetam (Standard)
    Inhibitor
    Levetiracetam (Standard) is the analytical standard of Levetiracetam. This product is intended for research and analytical applications. Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent.
    Levetiracetam (Standard)
  • HY-168088
    DNMT1/HDAC-IN-1
    Inhibitor
    DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities.
    DNMT1/HDAC-IN-1
  • HY-163614
    SARS-CoV-2-IN-87
    Inhibitor
    SARS-CoV-2-IN-87 (compound 138968421) is a potent inhibitor of methyltransferases (nsp14 and nsp16) of SARS-CoV-2.
    SARS-CoV-2-IN-87
  • HY-168346
    TS-002455
    TS-002455 (Example 668) is an inhibitor for Lin28a-dep Z11 with an IC50 < 1 μM. TS-002455 is the enantiomer of TS-002266 (HY-169091).
    TS-002455
  • HY-124588
    MC3343
    Inhibitor
    MC3343, a DNMT inhibitor (EC50 of 5.7 μM) and a strong DNA binder, affects tumor proliferation by blocking OS cells in G1 or G2/M phases and induces osteoblastic differentiation through the specific re-expression of genes regulating this physiological process.
    MC3343
  • 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
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