DNA methyltransferase (DNMT) including DNMT1, DNMT2, DNMT3A and DNMT3B are important enzymes for the DNA methylation patterns[3]. RG108 is a DNMT inhibitor with IC50 value of 115 nmol/L[4]. Human endometrial cancer ishikawa cells treated with different concentration from 5 - 40 μM RG108 for 72 hours. The cell proliferation was inhibited in a dose dependent manner and RG108 could significantly inhibit the viability as measured by MTT assay. The cell cycle was blocked in G2/M phase as detected by flow cytometry. The protein level of hLMH1 was increased and DNMT3B level was inhibited as measured by western blotting assay[5]. A tumor transplantation model in BALB/c mice was injected with 50 mg/kg of RG108 for 6 days followed by 8 Gy radiation after the last RG108 treatment. The tumor growth was inhibited significantly by the combination of RG108 and IR[6].
作用机制
The RG108 could block the active site of the DNMT1 enzyme and specifically depend on the carboxyl group[4].
RG108 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 HepG2 cells
Function assay
Inhibition of ACAT in human HepG2 cells, IC50=0.479 μM
19167888
human MCF7 cells
10 μM
Function assay
6 h
Induction of apoptosis in human MCF7 cells assessed as apoptotic cells at 10 uM after 6 hrs by FITC-Annexin V/propidium iodide staining-based FACS analysis relative to control
25801160
human THP1 cells
Function assay
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation, IC50=1.5 μM
18620381
rat macrophages
Function assay
24 h
Inhibition of ACAT in rat macrophages assessed as incorporation of extracellular [3H]-oleic acid-BSA complex into the intracellular cholesteryl ester after 24 hrs, IC50=0.479 μM
Inhibition of ACAT in human HepG2 cells, IC50=0.479 μM
19167888
human MCF7 cells
10 μM
Function assay
6 h
Induction of apoptosis in human MCF7 cells assessed as apoptotic cells at 10 uM after 6 hrs by FITC-Annexin V/propidium iodide staining-based FACS analysis relative to control
25801160
human THP1 cells
Function assay
Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation, IC50=1.5 μM
18620381
rat macrophages
Function assay
24 h
Inhibition of ACAT in rat macrophages assessed as incorporation of extracellular [3H]-oleic acid-BSA complex into the intracellular cholesteryl ester after 24 hrs, IC50=0.479 μM
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