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-B0464
    Hydralazine hydrochloride
    		Inhibitor 99.97%
    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
  • HY-101925
    CM-272
    		Inhibitor 98.70%
    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
  • HY-144433
    DNMT3A-IN-1
    		Inhibitor 99.94%
    DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with KI values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis).
    DNMT3A-IN-1
  • HY-162080
    METTL1-WDR4-IN-1
    		Inhibitor 99.61%
    METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking 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 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 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
  • HY-15229
    Guadecitabine sodium
    		Inhibitor 99.97%
    Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
    Guadecitabine sodium
  • HY-103397
    Nanaomycin A
    		Inhibitor 98.18%
    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. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
    Nanaomycin A
  • HY-A0084
    Procainamide hydrochloride
    		Inhibitor 99.52%
    Procainamide hydrochloride (Procaine amide hydrochloride) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research.
    Procainamide hydrochloride
  • HY-W012078
    5-Methyl-2'-deoxycytidine
    		99.87%
    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
  • HY-13668
    Lomeguatrib
    		Inhibitor 99.77%
    Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.
    Lomeguatrib
  • HY-A0084A
    Procainamide
    		Inhibitor 99.80%
    Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research.
    Procainamide
  • HY-B2194
    γ-Oryzanol
    		Inhibitor 99.66%
    γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
    γ-Oryzanol
  • HY-163385
    ALKBH1-IN-1
    		Inhibitor 99.63%
    ALKBH1-IN-1 (Compound 13h) is a selective ALKBH1 inhibitor, with an IC50 of 0.026 μM and 1.39 μM in the fluorescence polarization and enzyme activity assay, respectively. ALKBH1-IN-1 can modulate the level of DNA 6mA modifications. ALKBH1-IN-1 can be used to study the functions of ALKBH1 and DNA 6mA.
    ALKBH1-IN-1
  • HY-116217
    5-Fluoro-2'-deoxycytidine
    		99.66%
    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
  • HY-129079A
    TFMB-(S)-2-HG
    		99.79%
    TFMB-(S)-2-HG is a potent TET2 inhibitor. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG downregulates Wnt3a, β-catenin (intranuclear) protein expression. TFMB-(S)-2-HG inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML).
    TFMB-(S)-2-HG
  • HY-162082
    METTL1-WDR4-IN-2
    		Inhibitor 99.71%
    METTL1-WDR4-IN-2, an adenosine derivative, is a selective methyltransferase Like 1 (METTL1)-WDR4 inhibitor with an IC50 of 41 μM. METTL1-WDR4-IN-2 shows selectivity against METTL3-14 (IC50 of 958 μM) and METTL16 (IC50 of 208 μM). METTL1-WDR4-IN-2 can be used for the study of cancer.
    METTL1-WDR4-IN-2
  • HY-12746
    DC-05
    		Inhibitor 99.04%
    DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
    DC-05
  • 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-139015
    5-Aza-4'-thio-2'-deoxycytidine
    		Inhibitor 99.89%
    5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects.
    5-Aza-4'-thio-2'-deoxycytidine
  • HY-10586R
    5-Azacytidine (Standard)
    		Inhibitor
    5-Azacytidine (Standard) is the analytical standard of 5-Azacytidine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-117421A
    CM-579 trihydrochloride
    		Inhibitor
    CM-579 trihydrochloride 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 trihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
DNA Methyltransferase Isoform Comparison

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