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 (15):

Cat. No. Product Name Effect Purity
  • 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-A0004
    Decitabine Inhibitor 99.99%
    Decitabine is a cytosine analog and one potent inhibitor of DNA methyltransferase.
  • HY-13962
    SGI-1027 Inhibitor 99.77%
    SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively.
  • HY-13642
    RG108 Inhibitor 99.75%
    RG108 is a non-nucleoside inhibitor of DNA methyltransferase with IC50 of 115 nM.
  • 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-13542
    SGI-110 Inhibitor
    SGI-110 is a DNA methyltransferases (DNMT) inhibitor.
  • 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-13765
    6-Thioguanine Inhibitor
    6-Thioguanine(6-TG) belongs to the thiopurine family of drugs that also include mercaptopurine and azathioprine, which are examples of antimetabolites; a purine analogue of the nucleobase guanine.
  • HY-13668
    Lomeguatrib Inhibitor
    Lomeguatrib (PaTrin-2) is a modified guanine base, which can repress the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) with an IC50 value of 6 nM.
  • HY-12747
    DC_517 Inhibitor >98.0%
    DC_517 is a novel selective non-nucleoside inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 = 1.7 μM).
  • 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-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-B1109
    N-Acetylprocainamide Inhibitor 99.90%
    N-Acetylprocainamide is the N-acetylated metabolite of Procainamide, it is a Class III antiarrhythmic agent, whereas procainamide is a Class Ia antiarrhythmic drug.
  • HY-12746
    DC_05 Inhibitor
    DC_05 is a non-nucleoside DNMT1 inhibitor(IC50=10.3 uM) with low micromolar IC50 values and significant selectivity toward other AdoMet-dependent protein methyltransferases.
  • HY-13057
    Glucose-conjugated MGMT inhibitor Inhibitor
    O6BTG-C8-βGlu is a glucose-conjugated MGMT inhibitor with IC50 values of 32 nM in vitro and 10 nM on HeLa S3 cell; the parent compound O6BTG's IC50 is 9 nM(in vitro).
Isoform Specific Products

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