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-180540
    MGMT-IN-1
    		Inhibitor
    MGMT-IN-1 (Compound 2) is a light-activated MGMT inhibitor. MGMT-IN-1 can effectively enhance the cytotoxicity of Temozolomide (TMZ) (HY-17364) only under light conditions, significantly increasing the DNA damage caused by TMZ. MGMT-IN-1 can be used for the study of chordoma.
    MGMT-IN-1
  • HY-151445
    ZIKV-IN-2
    		Inhibitor
    ZIKV-IN-2 (compound 3a) is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 38.86 μM. ZIKV-IN-2 inhibits ZIKV replication and infection. ZIKV-IN-2 can be used in research of Zika virus (ZIKV).
    ZIKV-IN-2
  • HY-13642G
    RG108 (GMP)
    		Inhibitor
    RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
    RG108 (GMP)
  • HY-176230
    DNMT-IN-5
    		Inhibitor
    DNMT-IN-5 is a stable and efficient DNA methyltransferase (DNMT) inhibitor with high stability and high activity with an IC50 of 0.78 nM. DNMT-IN-5 exhibits sub-micromolar DNMT3A inhibitory activity, upregulates the expression of DNMT-targeted genes, impairs cell proliferation, and triggers a critical cell cycle arrest. DNMT-IN-5 can be used for the study of p53-depleted colorectal cancer.
    DNMT-IN-5
  • HY-175299
    Hedgehog IN-11
    		Inhibitor
    Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).
    Hedgehog IN-11
  • HY-133030
    DNMT-IN-1
    		Inhibitor
    DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active.
    DNMT-IN-1
  • HY-183852
    GSK3830052
    		Inhibitor
    GSK3830052 is a selective DNA methyltransferase 1 (DNMT1) inhibitor. GSK3830052 can be used to study cancer, sickle cell disease, β-thalassemia, and other diseases associated with DNMT1 inhibition.
    GSK3830052
  • 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-182956
    DNMT1 Degrader-1
    		Degrader
    DNMT1 Degrader-1 is a selective DNMT1 degrader with an IC50 of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia.
    DNMT1 Degrader-1
  • 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-182309
    SC83288
    		Inhibitor
    SC83288 is a Plasmodium falciparum PfDNMT2 inhibitor with an IC50 of 7 μM. SC83288 disrupts the epigenetic regulation of malaria parasites, blocks DNA replication and nuclear division, arrests the development of the asexual blood stage, induces the formation of pyknotic morphology in malaria parasites, and does not affect cytokinesis after nuclear division or parasite egress. SC83288 is applicable to malaria-related research.
    SC83288
  • HY-E70212
    Hhal Methyltransferase
    Hhal Methyltransferase (Hhal) is a DNA methyltransferase (recognition sequence: GCGC).
    Hhal Methyltransferase
  • HY-13689G
    Go 6983 (GMP)
    		Inhibitor
    Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.
    Go 6983 (GMP)
  • 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-148914
    S-Tubercidinylhomocysteine
    		Inhibitor
    (S)-Tubercidinylhomocysteine (Page 46) is a potent inhibitor of S-adenosylmethionine-dependent methyltransferase. (S)-Tubercidinylhomocysteine can be used for the study of herpesviruses (HSV) and vaccinia (VV).
    S-Tubercidinylhomocysteine
Cat. No. Product Name / Synonyms Application Reactivity
DNA Methyltransferase Isoform Comparison

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