货号：A9354

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

DNA methyltransferase enzymes (DNMTs) are responsible for the DNA methylation process which could catalyze the transfer of a methyl group from S-adenosyl methionine to the cytosine target nucleotide producing methylcytosine. Azacytidine (5-AZ) is a DNMT inhibitor with IC50 value of 0.8 - 3 μmol/L on MM cells. The K12-72.1 cells were treated with 5-AZ at both 5 and 10 μM, and the methylation status of the CpG sites in the promotor region of the gene PGP9.5 were measured by bisulfite sequencing. It was found that both concentrations could cause demethylation of the CpG sites and increased the expression of the gene PGP9.5. Moreover, after the treatment of 50 μM of 5-AZ on MCF10CA1a and MCF7 cells, the cell viability as measured by MTT assay decreased significantly compared with control. The nude mice with SKOV3 xenografts were treated with 2 mg/kg 5-AZ thrice weekly for 10 weeks. The volume and weight per nodule were decreased after the treatment of 5-AZ, which indicated that the 5-AZ could inhibit growth of tumors.

作用机制

The 5-AZ could inhibit the DNA methylation through covalently binding to DNA methyltransferases, forming nucleoprotein adducts. Therefore, the number of active DNA methyltransferase enzymes in the cells are depletes.

产品信息