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CAS No.: 48208-26-0

RG108/N-酞酰-L-色氨酸 Catalog No. CSN16078

Synonyms: N-Phthalyl-L-tryptophan

RG108 is a DNA methyltransferase inhibitor with IC50 of 115 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DNA Methyltransferase

IC50:115nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Mice: 5.69 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5.69 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9911 mL
- 14.9555 mL
- 29.9110 mL
- 5 mM
- 0.5982 mL
- 2.9911 mL
- 5.9822 mL
- 10 mM
- 0.2991 mL
- 1.4955 mL
- 2.9911 mL

技术信息

CAS号

48208-26-0

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H14N2O4

运输

蓝冰

分子量

334.33

别名

N-Phthalyl-L-tryptophan

溶解度

DMSO	67.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	66.0 mg/mL (197.4 mM)

动物实验配方

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