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.
DNA methylation on the cytosine of CpGdinucleotides in gene promoter regions is associated with silencing gene expression. Of the DNA methyltransferases, only DNA methyltransferase 3a (DNMT3a) and 3b (DNMT3b) are capable of adding de novo CpG methylation marks and thus may dynamically regulate gene silencing.
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Bobcat339 (Bobcat 339) is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a; Bobcat339 is a useful tool for investigation of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription.
A novel DNA hypomethylating dinucleotide that inhibits DNA methyltransferase (DNMT); induces/up-regulates the expression of investigated cancer/testis antigens in broad cancer cell lines, both at mRNA and at protein levels; reduces the stem-like properties of ALDH(+) ovarian cancer stem-like cells, including their tumor-initiating capacity, resensitizes these OCSCs to platinum; induces hypomethylation and CTA gene expression in a dose dependent manner both in vitro and in vivo.
DC_05 is a selective, non-nucleoside DNA methyltransferase DNMT1 inhibitor with IC50 of 10.3 uM, displays 3.6-fold selectivity over PRMT1 and >15-fold over DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9.
DC_05 is a potent, selective, non-nucleoside DNA methyltransferase DNMT1 inhibitor with IC50 of 1.7 uM, displays significant selectivity toward other AdoMet-dependent protein methyltransferases; significantly inhibits cancer cell proliferation in vitro.
SGI-1027 (SGI1027) is a potent inhibitor of DNA methyltransferase (DNMT) with IC50s of 6-12.5 uM for DNMT1, DNMT3A, and DNMT3B; induces selective degradation of DNMT1 with minimal or no effects on DNMT3A and DNMT3B in different cancer cell lines.
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; displays increased potency against DNMT1 compared with RG-108 and SGI-1027; efficiently inhibits OS cell proliferation and induces osteoblastic differentiation, induces dose- and time-dependent decreases in DNMT1, DNMT3a and DNMT3b protein levels in Saos-2 OS cells; displays synergistic effects with doxorubicin and cisplatin in vivo, reduces patient-derived xenograft OS growth and induces differentiation.
AA-CW236 (AA-CW-236;AA-CW 236) is a potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency; exhibits a high degree of selectivity towards MGMT, strongly sensitizes the effect of DNA alkylating drug temozolomide in breast and colon cancer cells by fluorescence imaging and a cell-viability assay.
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