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-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-124588
    MC3343
    		Inhibitor 98.14%
    MC3343, a DNMT inhibitor (EC50 of 5.7 μM) and a strong DNA binder, affects tumor proliferation by blocking OS cells in G1 or G2/M phases and induces osteoblastic differentiation through the specific re-expression of genes regulating this physiological process.
    MC3343
  • HY-N11722
    Panduratin A
    		Inhibitor 99.9%
    Panduratin A is an orally active natural compound with multiple pharmacological activities. By specifically inhibiting the NF-κB signaling pathway, Panduratin A exerts potent anti-inflammatory and antioxidant effects in intestinal and vascular inflammation models. Panduratin A exerts a definite protective effect against Colistin (HY-113678)-induced nephrotoxicity by alleviating oxidative stress, improving mitochondrial dysfunction and inhibiting cell apoptosis. Panduratin A activates autophagy via an AMPK-dependent pathway and exhibits anti-tuberculosis activity. Panduratin A exerts antiviral effects by inhibiting the methyltransferase (DNA Methyltransferase) of SARS-CoV-2.
    Panduratin A
  • HY-170524
    TDI-015051
    		Inhibitor
    TDI-015051 is a highly selective, orally active antiviral agent that targets the coronavirus NSP14 guanine-N7 methyltransferase. TDI-015051 binds to substrates in a non-competitive manner and forms a stable ternary complex, precisely blocking the capping and methylation processes of viral mRNA. TDI-015051 potently inhibits a variety of coronaviruses (including SARS-CoV-2 and MERS). By impairing viral replication and translation and inducing a moderate type I interferon-mediated immune response, it significantly reduces pulmonary viral load and exhibits a synergistic effect with Nirmatrelvir (HY-138687). In addition, TDI-015051 does not inhibit non-coronavirus methyltransferases, and the drug-resistant mutations it induces impair viral fitness, demonstrating excellent antiviral properties and safety. TDI-015051 can be used for research on COVID-19 and the replication mechanism of coronaviruses.The IC50 values of TDI-015051 against SARS-CoV-2, α-hCoV-NL63, α-hCoV-229E, β-hCoV-MERS are 0.15 nM, 1.7 nM, 2.6 nM and 3.6 nM, respectively, and the Ka value against SARS-CoV-2 is 0.061 nM.
    TDI-015051
  • HY-111644
    6-Methyl-5-azacytidine
    		Inhibitor
    6-Methyl-5-azacytidine is a potent DNMT inhibitor.
    6-Methyl-5-azacytidine
  • HY-162080A
    METTL1-WDR4-IN-1 TFA
    		Inhibitor 99.61%
    METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8+ T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy.
    METTL1-WDR4-IN-1 TFA
  • 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-E70206
    CpG Methyltransferase
    CpG Methyltransferase is a DNA methyltransferase. CpG Methyltransferase can methylate the C5 position on the base moiety of all cytosine nucleotides contained in unmethylated or hemimethylated double stranded DNA in a 5’-CpG-3’ context.
    CpG Methyltransferase
  • HY-112551
    2′,3′,5′-Triacetyl-5-azacytidine
    		98.09%
    2′,3′,5′-Triacetyl-5-azacytidine is an orally active proagent of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase.
    2′,3′,5′-Triacetyl-5-azacytidine
  • HY-133021
    Arazine
    		98.0%
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
    Arazine
  • HY-P10407
    BM30
    		Inhibitor 99.45%
    BM30 is a selective peptidomimetic NTMT1 and NTMT2 inhibitor (IC50: 0.89 μM for NTMT1).
    BM30
  • HY-B0464S
    Hydralazine-d4 (hydrochloride)
    		Inhibitor
    Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.
    Hydralazine-d<sub>4</sub> (hydrochloride)
  • HY-W012078R
    5-Methyl-2'-deoxycytidine (Standard)
    5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells.
    5-Methyl-2'-deoxycytidine (Standard)
  • HY-168088
    DNMT1/HDAC-IN-1
    		Inhibitor
    DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities.
    DNMT1/HDAC-IN-1
  • HY-163614
    SARS-CoV-2-IN-87
    		Inhibitor
    SARS-CoV-2-IN-87 (compound 138968421) is a potent inhibitor of methyltransferases (nsp14 and nsp16) of SARS-CoV-2.
    SARS-CoV-2-IN-87
  • HY-179409A
    MC3817 free base
    		Inhibitor
    MC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and γH2AX. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.
    MC3817 free base
  • HY-168346
    TS-002455
    TS-002455 (Example 668) is an inhibitor for Lin28a-dep Z11 with an IC50 < 1 μM. TS-002455 is the enantiomer of TS-002266 (HY-169091).
    TS-002455
  • HY-177807
    DNMT1 aptamer sodium
    		Inhibitor
    DNMT1 aptamer sodium is a DNA aptamer for binding and inhibition of DNA methyltransferase 1 (DNMT1).
    DNMT1 aptamer sodium
  • 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
DNA Methyltransferase Isoform Comparison

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