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-129079A
    TFMB-(S)-2-HG
    99.62%
    TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML).
    TFMB-(S)-2-HG
  • HY-13668
    Lomeguatrib
    Inhibitor 99.63%
    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-15229
    Guadecitabine sodium
    Inhibitor 98.05%
    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-W012078
    5-Methyl-2'-deoxycytidine
    99.87%
    5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation.
    5-Methyl-2'-deoxycytidine
  • HY-A0084
    Procainamide hydrochloride
    Inhibitor ≥98.0%
    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-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
  • HY-161402
    METTL16-IN-1
    Inhibitor 99.22%
    METTL16-IN-1 (Compound 45) is a potent METTL16 inhibitor with an IC50 value of 1.7 μM and a Kd value of 1.35 μM.
    METTL16-IN-1
  • HY-162082
    METTL1-WDR4-IN-2
    Inhibitor 99.71%
    METTL1-WDR4-IN-2 (compound 6) is a selective methyltransferase Like 1 (METTL1)-WDR4 inhibitor with an IC50 of 41 μM. METTL1-WDR4-IN-2 shows remarkable selectivity against METTL3-14 and slightly selective also against METTL16.
    METTL1-WDR4-IN-2
  • HY-N2150
    Psammaplin A
    Inhibitor
    Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
    Psammaplin A
  • HY-150249
    GSK3735967
    Inhibitor 99.71%
    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-12747
    DC_517
    Inhibitor 99.67%
    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-12746
    DC-05
    Inhibitor 98.96%
    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-131991
    Benzyl selenocyanate
    Inhibitor ≥99.0%
    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-12310
    RSC133
    Inhibitor ≥98.0%
    RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells.
    RSC133
  • 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-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-139015
    5-Aza-4'-thio-2'-deoxycytidine
    Inhibitor 99.09%
    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-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-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
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