RG108

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Chemical Structure| 48208-26-0 同义名 : N-Phthalyl-L-tryptophan
CAS号 : 48208-26-0
货号 : A548158
分子式 : C19H14N2O4
纯度 : 99%+
分子量 : 334.325
MDL号 : MFCD08705332
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(314.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • DNA Methyltransferase

    DNA methyltransferase, IC50:115 nM
描述 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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.96mL

2.99mL

1.50mL

29.91mL

5.98mL

2.99mL
参考文献

[1]Oh YS, Jeong SG, Cho GW. Anti-senescence effects of DNA methyltransferase inhibitor RG108 in human bone marrow mesenchymal stromal cells. Biotechnol Appl Biochem. 2015 Sep-Oct;62(5):583-90.

[2]Graca I, Sousa EJ, et al. Anti-tumoral effect of the non-nucleoside DNMT inhibitor RG108 in human prostate cancer cells. Curr Pharm Des. 2014;20(11):1803-11.

[3]Bestor TH. The DNA methyltransferases of mammals. Hum Mol Genet. 2000 Oct;9(16):2395-402.

[4]Brueckner B, Garcia Boy R, Siedlecki P, Musch T, Kliem HC, Zielenkiewicz P, Suhai S, Wiessler M, Lyko F. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

[5]Yang L, Hou J, Cui XH, Suo LN, Lv YW. RG108 induces the apoptosis of endometrial cancer Ishikawa cell lines by inhibiting the expression of DNMT3B and demethylation of HMLH1. Eur Rev Med Pharmacol Sci. 2017 Nov;21(22):5056-5064.

[6]Ou Y, Zhang Q, Tang Y, Lu Z, Lu X, Zhou X, Liu C. DNA methylation enzyme inhibitor RG108 suppresses the radioresistance of esophageal cancer. Oncol Rep. 2018 Mar;39(3):993-1002.