DNA methylation, defined by the addition of a methyl group to adenine or cytosine bases in DNA catalyzed by DNA methyltransferases (MTases), is one of the most studied post-replicative DNA modification mechanism in bacteria. The three forms of nucleotide methylation identified to date are: N6-methyladenine(m6A), N4-methylcytosine (m4C), and 5-methylcytosine (m5C).DNA methylation, one type of epigenetic modification, represses gene expression. DNA methylation is caused primarily by a family of DNA methyltransferases (DNMTs) including DNMT1, DNMT3a and DNMT3b. Conventionally, DNMT1 acts as the primary maintenance methyltransferase to keep the methylation of DNA that is already established at the genome, whereas DNMT3a and DNMT3b are classified asde novo methyltransferases to reversibly methylate unmethylated DNA. DNA methylation represses gene transcription through several mechanisms including physically blocking the binding of transcription factors and/or functioning as docking sites for transcriptional repressors/corepressors.In epigenetic transcriptional regulation, which is important for embryonic development, DNA-methylation patterns are determined by de novo methylation by the DNA methyltransferases Dnmt3a and Dnmt3b in the embryo.
||RG108 is a non-nucleoside inhibitor of DNA methyltransferase with IC50 of 115 nM.
||SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively.
||6-Thioguanine(6-TG) belongs to the thiopurine family of drugs that also include mercaptopurine and azathioprine, which are examples of antimetabolites; a purine analogue of the nucleobase guanine.
||Glucose-conjugated MGMT inhibitor
||O6BTG-C8-βGlu is a glucose-conjugated MGMT inhibitor with IC50 values of 32 nM in vitro and 10 nM on HeLa S3 cell; the parent compound O6BTG's IC50 is 9 nM(in vitro).
||SGI-110 is a DNA methyltransferases (DNMT) inhibitor.
||A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.
||MC3343 (MC-3343) is a novel potent, non-nucleoside DNA methyltransferase (DNMT) inhibitor with IC50 of 5.7 and 1.7 uM for DNMT1 and DNMT3a in cell-free assays, respectively.