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DNA Methyltransferase

DNA methyltransferases (DNMTs) are a family of enzymes that catalyze the transfer of a methyl group from the methyl donor, usually S-adenosyl-L-methionine (SAM) for all known DNMTs, to the 5-position of cytosine residues in DNA. In mammals, four members of the DNMT gene family have been identified and designated, DNMT1, DNMT3A, DNMT3B and DNMT3L respectively, in which DNMT1 encodes the maintenance methyltransferase, DNMT3A/3B encode the de novo methyltransferases, and DNMT3L encodes an enzyme without any inherent enzymatic activity. Mammalian DNMTs are involved in transcriptional silencing of several sequence classes and play an important role in maintaining genome stability and genomic integrity.

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  1. Cat.No. Product Name Information
  2. A8191 Nanaomycin A Nanaomycin A is a selective inhibitor of DNA methyltransferase 3B (DNMT3B) with IC50 value of 500 nM .
  3. A4176 Thioguanine Thioguanine is a purine antimetabolite widely used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.
  4. A1915 Zebularine Zebularine, a chemically stable cytidine analog containing a 2-(1H)-pyridimidinone ring, is an effective DNA methylation inhibitor which can act with DNA methyltransferases to form a covalent complex. It has been shown to cause demethylation and reactivation of a silenced and hypermethylated p16 gene.
  5. A1913 RG 108 RG108 is a DNA methyltransferase (DMNT) inhibitor that enhanced reprogramming of OK-transduced MEFs in the presence of BIX.
  6. A1912 Lomeguatrib Inhibitor of O6-methylguanine-DNA methyltransferase (MGMT); (IC50 = 0.009 μM in cell-free extracts from HeLa S3 cells);
  7. A1907 5-Azacytidine 5-Azacytidine (also known as 5-AzaC), a compound belonging to a class of cytosine analogues, is a DNA methyl transferase (DNMT) inhibitor that exerts potent cytotoxicity against multiple myeloma (MM) cells, including MM.1S, MM.1R, RPMI-8266, RPMI-LR5, RPMI-Dox40 and Patient-derived MM, with the half maximal inhibition concentration IC50 values of 1.5 μmol/L, 0.7 μmol/L, 1.1 μmol/L, 2.5 μmol/L, 3.2 μmol/L and 1.5 μmol/L respectively .
  8. A1906 Decitabine (NSC127716, 5AZA-CdR) Decitabine is a kind of deoxycytidine analog and an inducer of cellular differentiation.
  9. C4119 2',3',5'-triacetyl-5-Azacytidine
  10. A8901 Nanaomycin C Nanaomycin C
  11. A4178 SGI-110 SGI-110 is a second generation DNA methyltransferase (DNMT) inhibitor that is synthesized as a dinucleotide consisting of a deoxyguanosine (5’-DACpG-3’) and 5-AZA-CdR bonds with a natural phosphodiester linkage. Unlike other DNMT inhibitors that are susceptible to rapid inactivation by cytidine deaminase (CDA), SGI-110 is highly resistant to deamination by CDA. In previous studies, SGI-110 has been demonstrated to effectively retard tumor growth in human bladder cancer xenografts through both intraperitoneal (i.p.) and subcutaneous (s.c.) administration and to exhibit epigenetic remodeling activity, in which the expression of p16 in cancer cells is restored through demethylation of the 5’-end region of the gene.

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