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-151136
    DY-46-2
    Inhibitor 99.32%
    DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM.
    DY-46-2
  • HY-13668
    Lomeguatrib
    Inhibitor 99.70%
    Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells.
    Lomeguatrib
  • HY-W012078
    5-Methyl-2'-deoxycytidine
    99.24%
    5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation.
    5-Methyl-2'-deoxycytidine
  • HY-129079A
    TFMB-(S)-2-HG
    99.62%
    TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML).
    TFMB-(S)-2-HG
  • HY-117421A
    CM-579 trihydrochloride
    Inhibitor 98.03%
    CM-579 trihydrochloride 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 trihydrochloride
  • HY-12747
    DC_517
    Inhibitor 99.67%
    DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
    DC_517
  • HY-150249
    GSK3735967
    Inhibitor 99.71%
    GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC50 value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3.
    GSK3735967
  • HY-139664A
    (R)-GSK-3685032
    Inhibitor 98.02%
    (R)-GSK-3685032 is the R-enantiomer of GSK-3685032. 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.
    (R)-GSK-3685032
  • 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-12746
    DC-05
    Inhibitor 99.08%
    DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
    DC-05
  • HY-131991
    Benzyl selenocyanate
    Inhibitor ≥99.0%
    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-12310
    RSC133
    Inhibitor ≥98.0%
    RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells.
    RSC133
  • HY-103397
    Nanaomycin A
    Inhibitor 98.18%
    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. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
    Nanaomycin A
  • 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-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-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-123346
    SW155246
    Inhibitor 98.31%
    SW155246 is a DNA methyltransferase (DNMT1) selective inhibitor with IC50s of 1.2 and 38 μM for hDNMT1 and mDNMT3A, respectively. SW155246 can be used for the research of cancer and other diseases.
    SW155246
  • 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
Cat. No. Product Name / Synonyms Application Reactivity

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