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.
DNA Methyltransferase Isoform Specific Products
All Product Categories
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DNA Methyltransferase Related Products (144)
Related Products (144)
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Antibodies (11)
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DNA Methyltransferase Isoform Comparison
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Hydralazine hydrochloride
0 ImagesHydralazine 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.
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CM-272
0 ImagesCM-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.
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DNMT3A-IN-1
0 ImagesDNMT3A-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).
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METTL1-WDR4-IN-1
0 ImagesMETTL1-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.
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Nanaomycin A
0 ImagesNanaomycin A is a selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A inhibits the in vitro growth of human Plasmodium falciparum with an IC80 of 33.1 nM.
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5-Methyl-2'-deoxycytidine
0 ImagesSynonyms: 5-Methyldeoxycytidine5-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.
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Guadecitabine sodium
0 ImagesSynonyms: SGI-110 sodium; S-110 sodiumGuadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
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Procainamide hydrochloride
0 ImagesSynonyms: Procaine amide hydrochloride; SP 100 hydrochlorideProcainamide 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.
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Procainamide
0 ImagesProcainamide (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.
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ALKBH1-IN-1
0 ImagesCat. No.: HY-163385Purity: 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.
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5-Fluoro-2'-deoxycytidine
0 ImagesSynonyms: FdCyd; NSC-480065-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.
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TFMB-(S)-2-HG
0 ImagesTFMB-(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).
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DC-05
0 ImagesDC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
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5-Azacytidine (Standard)
0 ImagesSynonyms: Azacitidine (Standard); 5-AzaC (Standard); Ladakamycin (Standard)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.
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5-Aza-4'-thio-2'-deoxycytidine
0 ImagesSynonyms: 5-Aza-T-dCyd; NTX-3015-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.
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CM-579 trihydrochloride
0 ImagesCat. No.: HY-117421ACAS No.: 2448471-08-5CM-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.
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Hydralazine
0 ImagesHydralazine 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.
