2. Signaling Pathways
  3. Epigenetics
  4. DNA Methyltransferase

DNA Methyltransferase

DNMTs; DNA MTases

DNA Methyltransferase

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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.

DNA Methyltransferase Isoform Specific Products:

DNA Methyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-172180
    DNMT-IN-4
    		Inhibitor
    DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 of 5.78 µM. DNMT-IN-4 can induce apoptosis and has anticancer activity.
    DNMT-IN-4
  • 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
  • HY-139137
    N-Acetyl-S-geranylgeranyl-L-cysteine
    		Inhibitor
    N-Acetyl-S-geranylgeranyl-L-cysteine is a Methyltransferase inhibitor. N-Acetyl-S-geranylgeranyl-L-cysteine inhibits beta 2 integrin-induced actin polymerization with an IC50 of 45 nM.
    N-Acetyl-S-geranylgeranyl-L-cysteine
  • HY-E70212
    Hhal Methyltransferase
    Hhal Methyltransferase (Hhal) is a DNA methyltransferase (recognition sequence: GCGC).
    Hhal Methyltransferase
  • HY-173002
    MS9024
    		Degrader
    MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM.
    MS9024
  • HY-163803
    CM-444
    		Inhibitor
    CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
    CM-444
  • HY-E70210
    GpC Methyltransferase
    GpC Methyltransferase (GpC) is a DNA methylating enzyme. GpC Methyltransferase methylates cytosines in GpC dinucleotides in non-nucleosomal DNA in vitro.
    GpC Methyltransferase
  • HY-116217R
    5-Fluoro-2'-deoxycytidine (Standard)
    5-Fluoro-2'-deoxycytidine (Standard) is the analytical standard of 5-Fluoro-2'-deoxycytidine. This product is intended for research and analytical applications. 5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity.
    5-Fluoro-2'-deoxycytidine (Standard)
  • HY-103397R
    Nanaomycin A (Standard)
    		Inhibitor
    Nanaomycin A (Standard) is the analytical standard of Nanaomycin A. This product is intended for research and analytical applications. Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].
    Nanaomycin A (Standard)
  • HY-13642A
    (Rac)-RG108
    		Inhibitor
    (Rac)-RG108 (NSC401077), a DNMT1 inhibitor, inhibits DNA methyltransferases.
    (Rac)-RG108
  • HY-119054
    DNMT1-IN-4
    		Inhibitor
    DNMT1-IN-4 is a potent non-nucleoside DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 2.5 µM and selectivity towards other AdoMet-dependent protein methyltransferases. DNMT1-IN-4 significantly inhibits cancer cell proliferation.
    DNMT1-IN-4
  • 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-B0106S1
    Levetiracetam-d3
    		Inhibitor
    Levetiracetam-d3 is the deuterium labeled Levetiracetam. 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-d<sub>3</sub>
  • HY-13786
    O6BTG-C8-αGlu
    		Inhibitor
    O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, O6BTG-C8-αGlu can completely inhibit MGMT in HeLaS3 cells. Even when applied chronically at high doses (up to 20 μM), it does not exhibit cytotoxicity. O6BTG-C8-αGlu is suitable for research on MGMT-related cancer diseases.
    O6BTG-C8-αGlu
  • HY-W653970
    5-Azacytidine-15N4
    		Inhibitor
    5-Azacytidine-15N4 is 13C and 15N labeled 5-Azacytidine. 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-<sup>15</sup>N<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
DNA Methyltransferase Isoform Comparison

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