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-116217R
    5-Fluoro-2'-deoxycytidine (Standard)
    5-Fluoro-2'-deoxycytidine (Standard) is the analytical standard of 5-Fluoro-2'-deoxycytidine. This product is intended for research and analytical applications. 5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity.
    5-Fluoro-2'-deoxycytidine (Standard)
  • HY-103397R
    Nanaomycin A (Standard)
    Inhibitor
    Nanaomycin A (Standard) is the analytical standard of Nanaomycin A. This product is intended for research and analytical applications. Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].
    Nanaomycin A (Standard)
  • HY-13642A
    (Rac)-RG108
    Inhibitor
    (Rac)-RG108 (NSC401077), a DNMT1 inhibitor, inhibits DNA methyltransferases.
    (Rac)-RG108
  • HY-119054
    DNMT1-IN-4
    Inhibitor
    DNMT1-IN-4 is a potent non-nucleoside DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 2.5 µM and selectivity towards other AdoMet-dependent protein methyltransferases. DNMT1-IN-4 significantly inhibits cancer cell proliferation.
    DNMT1-IN-4
  • 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-101925R
    CM-272 (Standard)
    Inhibitor
    CM-272 (Standard) is the analytical standard of CM-272 (HY-101925). This product is intended for research and analytical applications. CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
    CM-272 (Standard)
  • HY-B0106S1
    Levetiracetam-d3
    Inhibitor
    Levetiracetam-d3 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.
    Levetiracetam-d<sub>3</sub>
  • HY-181963
    ZINC-1000507824
    ZINC-1000507824 is a non-covalent reversible RNA cytosine-5 methyltransferase NSUN2 inhibitor. ZINC-1000507824 targets the SAM cofactor binding pocket of NSUN2 and forms stable NSUN2-ligand complexes. ZINC-1000507824 destabilizes oncogenic mRNAs encoding PI3K/AKT and MAPK/ERK pathway components, attenuates growth signals, reduces proliferative drive, and restores therapy sensitivity in cancer cells. ZINC-1000507824 can be used for the research of NSUN2-driven malignancies.
    ZINC-1000507824
  • HY-13786
    O6BTG-C8-αGlu
    Inhibitor
    O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, O6BTG-C8-αGlu can completely inhibit MGMT in HeLaS3 cells. Even when applied chronically at high doses (up to 20 μM), it does not exhibit cytotoxicity. O6BTG-C8-αGlu is suitable for research on MGMT-related cancer diseases.
    O6BTG-C8-αGlu
  • HY-B0464R
    Hydralazine hydrochloride (Standard)
    Inhibitor
    Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. 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 hydrochloride (Standard)
  • HY-W653970
    5-Azacytidine-15N4
    Inhibitor
    5-Azacytidine-15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
    5-Azacytidine-<sup>15</sup>N<sub>4</sub>
  • HY-B2230R
    Hinokitiol (Standard)
    Inhibitor
    Hinokitiol (Standard) is the analytical standard of Hinokitiol. This product is intended for research and analytical applications. Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
    Hinokitiol (Standard)
  • HY-A0084R
    Procainamide hydrochloride (Standard)
    Inhibitor
    Procainamide (hydrochloride) (Standard) is the analytical standard of Procainamide (hydrochloride). This product is intended for research and analytical applications.
    Procainamide hydrochloride (Standard)
  • HY-160084
    2′-Deoxy-4′-thiocytidine
    Inhibitor
    2′-Deoxy-4′-thiocytidine (T-dCyd) is a novel epigenetic agent. 2′-Deoxy-4′-thiocytidine administrations led to a significant p21 increase. 2′-Deoxy-4′-thiocytidine can eradicate of tumor cells in the double-mutant xenografts.
    2′-Deoxy-4′-thiocytidine
  • HY-A0004S
    Decitabine-13C5
    Inhibitor
    Decitabine-13C5 (5-Aza-2'-deoxycytidine-13C5) is 13C labeled Decitabine. 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-<sup>13</sup>C<sub>5</sub>
  • HY-179048
    MH44
    Inhibitor
    MH44 is an efficient inhibitor targeting the SARS-CoV-2 nsp14 N7-methyltransferase (N7-MTase) with an IC50 of 19 nM. MH44 exhibits moderate antiviral effects in SARS-CoV-2-infected A549-hACE2 cells and shows certain cytotoxicity at higher concentrations. MH44 can be used in the research on anti-SARS-CoV-2.
    MH44
  • HY-135043
    S-Aristeromycinyl-L-homocysteine
    Inhibitor
    S-Aristeromycinyl-L-homocysteine is an S-adenosylmethionine-dependent methyltransferase inhibitor.
    S-Aristeromycinyl-L-homocysteine
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