1. Epigenetics
  2. DNA Methyltransferase

DNA Methyltransferase

DNA methylation, defined by the addition of a methyl group to adenine or cytosine bases in DNA catalyzed by DNA methyltransferases (MTases), is one of the most studied post-replicative DNA modification mechanism in bacteria. The three forms of nucleotide methylation identified to date are: N6-methyladenine(m6A), N4-methylcytosine (m4C), and 5-methylcytosine (m5C).

DNA methylation, one type of epigenetic modification, represses gene expression. DNA methylation is caused primarily by a family of DNA methyltransferases (DNMTs) including DNMT1, DNMT3a and DNMT3b. Conventionally, DNMT1 acts as the primary maintenance methyltransferase to keep the methylation of DNA that is already established at the genome, whereas DNMT3a and DNMT3b are classified asde novo methyltransferases to reversibly methylate unmethylated DNA. DNA methylation represses gene transcription through several mechanisms including physically blocking the binding of transcription factors and/or functioning as docking sites for transcriptional repressors/corepressors.

In epigenetic transcriptional regulation, which is important for embryonic development, DNA-methylation patterns are determined by de novo methylation by the DNA methyltransferases Dnmt3a and Dnmt3b in the embryo.

DNA methylation on the cytosine of CpGdinucleotides in gene promoter regions is associated with silencing gene expression. Of the DNA methyltransferases, only DNA methyltransferase 3a (DNMT3a) and 3b (DNMT3b) are capable of adding de novo CpG methylation marks and thus may dynamically regulate gene silencing.

DNA Methyltransferase Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-A0004
    Decitabine Inhibitor 99.99%
    Decitabine is a cytosine analog and one potent inhibitor of DNA methyltransferase.
  • HY-10586
    5-Azacytidine Inhibitor 99.97%
    5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.
  • HY-13962
    SGI-1027 Inhibitor 99.77%
    SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
  • HY-13420
    Zebularine Inhibitor 99.92%
    Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor; also an inhibitor of cytidine deaminase with a Ki of 0.95 μM.
  • HY-13642
    RG108 Inhibitor 99.75%
    RG108 is a non-nucleoside inhibitor of DNA methyltransferase with IC50 of 115 nM.
  • HY-15229
    Guadecitabine sodium Inhibitor
    S-110 is a dinucleotide consisting of 5-Aza-CdR followed by a deoxyguanosine which shows to be an effective DNA methylation inhibitor.
  • HY-13542
    SGI-110 Inhibitor 98.00%
    SGI-110 is a DNA methyltransferases (DNMT) inhibitor.
  • HY-13668
    Lomeguatrib Inhibitor
    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.
  • HY-12747
    DC_517 Inhibitor >98.0%
    DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
  • HY-B2230
    Hinokitiol Inhibitor >98.0%
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-B2194
    γ-Oryzanol Inhibitor
    γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
  • HY-12746
    DC-05 Inhibitor 99.15%
    DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
  • HY-13057
    Glucose-conjugated MGMT inhibitor Inhibitor
    Glucose-conjugated MGMT inhibitor 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.