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-B0464A
    Hydralazine
    		Inhibitor 99.94%
    Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine 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
  • HY-12747
    DC_517
    		Inhibitor 99.33%
    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-139664A
    (R)-GSK-3685032
    		Inhibitor 98.97%
    (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-123346
    SW155246
    		Inhibitor 98.04%
    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-N2150
    Psammaplin A
    		Inhibitor
    Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM) and aminopeptidase N (APN) (IC50: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis.
    Psammaplin A
  • HY-135146A
    (Rac)-GSK-3484862
    		Control 98.76%
    (Rac)-GSK-3484862 is the isomer of GSK-3484862 (HY-135146), and can be used as an experimental control. GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
    (Rac)-GSK-3484862
  • HY-158075
    DNMT/HDAC-IN-1
    		Inhibitor 99.87%
    DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.
    DNMT/HDAC-IN-1
  • HY-150249
    GSK3735967
    		Inhibitor 99.34%
    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-13765R
    6-Thioguanine (Standard)
    		Inhibitor
    6-Thioguanine (Standard) is the analytical standard of 6-Thioguanine. This product is intended for research and analytical applications. 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
    6-Thioguanine (Standard)
  • HY-12310
    RSC133
    		Inhibitor 98.45%
    RSC133 is a dual inhibitor of DNA methyltransferase 1 and histone deacetylase 1 inhibitor. RSC133 promotes cell proliferation, up-regulates H3K9 histone acetylation, down-regulates p53, p21, p16/INK4A, and ablates pro-senescence phenotypes.
    RSC133
  • HY-B0106R
    Levetiracetam (Standard)
    		Inhibitor
    Levetiracetam (Standard) is the analytical standard of Levetiracetam. This product is intended for research and analytical applications. Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent.
    Levetiracetam (Standard)
  • 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-126426
    CBHcy
    		Inhibitor 99.95%
    CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model.
    CBHcy
  • HY-131991
    Benzyl selenocyanate
    		Inhibitor 99.85%
    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-119390
    AA-CW236
    		Inhibitor 99.9%
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification.
    AA-CW236
  • HY-139664B
    (S)-GSK-3685032
    		Inhibitor 98.82%
    (S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. 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.
    (S)-GSK-3685032
  • HY-175594
    DNMT2-IN-2
    		Inhibitor 99.13%
    DNMT2-IN-2 is a selective DNA methyltransferase 2 (DNMT2) inhibitor with a KD value of 3.04 μM. DNMT2-IN-2 targets to a cryptic allosteric binding site of DNMT2. DNMT2-IN-2 reduces m5C levels in MOLM-13 tRNA and synergizes with Doxorubicin (HY-15142A) to impair cell viability. DNMT2-IN-2 can be used for cancer research, such as cervical cancer and leukemia.
    DNMT2-IN-2
  • HY-173002
    MS9024
    		Degrader 99.83%
    MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM.
    MS9024
  • HY-W740027
    5-Methyl-2'-deoxycytidine-d3
    		98.94%
    5-Methyl-2'-deoxycytidine-d3 (5-Methyldeoxycytidine-d3) is the deuterium labeled Methyl-2'-deoxycytidine (HY-W012078). 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-d<sub>3</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
DNA Methyltransferase Isoform Comparison

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