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[3]. SGI-1027 is a DNMT inhibitor with IC50 value of 0.8 µM and 10 µM on DNMT3Acat and DNMT1, respectively[4]. The RKO cells were treated with SCI-1027 at 2.5 µmol/L. The P16, MLH1 level measured by RT-PCR was reactivated after the treatment for 7 days. The protein level of P16 and TIMP3 measured by western blotting assay were also increased after 12 days of treatment while the level of DNMT1 was inhibited[5]. The cell viability of the human HCC cell line decreased in a dose dependent manner from 5 - 30 µmol after the treatment of SGI-1027 for 24 hours[6]. The C57BL/6J mice were intravitreally administered SGI-1027 10 μM in 2 μl, 24 hours before retinal injury. Only in the GLAST-positive fractions, the Oct4 expression measured by western blotting assay could be sustained after the treatment of SGI-1027[7].
作用机制
The SGI-1027 could inhibit the DNMT activity by inducing the degradation of the DNMT1 and reactivating the TSGs. It cannot bind to the RNA or the minor groove of DNA[6].
SGI-1027 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human HCT116 cells
Cytotoxicity assay
Cytotoxicity against human HCT116 cells assessed as viability, TD50=25 μM
23639684
human KARPAS299 cells
Proliferation assay
2-4 days
Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay, EC50=1.8 μM
26220519
human KG1 cells
Proliferation assay
2-4 days
Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay, EC50=4.4 μM
26220519
human MDA-MB-231 cells
Cytotoxicity assay
48 h
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay, IC50=4.8 μM
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