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- A9354
- 2026年01月10日
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- 库存：
9999
- 规格：
100mg
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
CAS号 |
320-67-2 |
|
分子式 |
C8H12N4O5 |
|
分子量 |
244.20 |
|
溶解度 |
DMSO |
32.0 mg/mL (131.0 mM) |
Ethanol |
insoluble |
|
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文献和实验5′-Azacytidine Expression Arrays
Epigenetic silencing of a gene can be reversed, resulting in reactivation of expression, by drugs such as the DNA methylation inhibitor 5-Aza-2′-deoxycytidine (5Aza-dC, azacytidine). This drug is added to cell culture media and is incorporated
Epigenetic Regulation of MicroRNA Expression in Cancer
. To identify miRs that are regulated by epigenetic mechanisms in cancer, we performed expression profiling prior to and following treatment of cell lines with 5-azacytidine. We used oligonucleotide microarrays to determine miR expression. For miRs
第一个DNA甲基转移酶抑制剂(5-阿扎西替丁)在1964年首次合成，其作为抗癌剂的潜力很早就被认识到。20世纪80年代，在临床对这些制剂的最初研究中，将地西他滨作为经典的抗癌药物，其剂量为临床最大耐受剂量，每疗程1500 - 2500 mg/m(2)，但收效甚微。只有当低剂量(那些没有细胞毒性,导致epigenetically沉默沉默基因的活化)取得任何重大进展,经过近40年5-azacytidine (Vidaza)最后获得FDA的批准在2004/2005专门治疗骨髓增生异常综合征(MDS
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