1. Signaling Pathways
  2. Epigenetics
  3. DNA Methyltransferase

DNA Methyltransferase

DNMTs; DNA MTases

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-123346
    SW155246
    Inhibitor 98.31%
    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-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-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-A0004R
    Decitabine (Standard)
    Inhibitor
    Decitabine (Standard) is the analytical standard of Decitabine. This product is intended for research and analytical applications. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
    Decitabine (Standard)
  • HY-111644
    6-Methyl-5-azacytidine
    Inhibitor
    6-Methyl-5-azacytidine is a potent DNMT inhibitor.
    6-Methyl-5-azacytidine
  • 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-119390
    AA-CW236
    Inhibitor 99.86%
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification.
    AA-CW236
  • 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-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-124588
    MC3343
    Inhibitor
    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-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
  • 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-19826
    Isofistularin-3
    Inhibitor
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
    Isofistularin-3
  • HY-162282
    PROTAC METTL3-14 degrader 1
    Degrader
    PROTAC METTL3-14 degrader 1 (compound 30) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14(Pink: Ligand for target protein (HY-115717); Black: Linker (HY-168686); Blue: Ligand for E3 ligase (HY-10984)).
    PROTAC METTL3-14 degrader 1
  • HY-161694
    DNMT1-IN-3
    Inhibitor
    DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor.
    DNMT1-IN-3
  • HY-B0106S
    Levetiracetam-d6
    Inhibitor
    Levetiracetam-d6 is the deuterium labeled Levetiracetam. 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[1][2].
    Levetiracetam-d<sub>6</sub>
  • HY-N12612
    CNP0296775
    Inhibitor
    CNP0296775 is an inhibitor of dengue virus methyltransferase (DENV MTase) that has the potential to disrupt the viral replication process.
    CNP0296775
  • HY-163535
    J208
    Inhibitor
    J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs).
    J208
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