RG 108
(Synonyms: N-Phthalyl-L-tryptophan,RG108) 目录号 : GC13398
DNA methyltransferase inhibitor
Cas No.:48208-26-0
Sample solution is provided at 25 µL, 10mM.
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RG108 is a DNA methyltransferase (DMNT) inhibitor that enhanced reprogramming of OK-transduced MEFs in the presence of BIX. It is a small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. DNA methylation regulates gene expression in normal and malignant cells. DNA methyltransferase inhibitors are able to reactivate epigenetically silenced genes. RG108 caused demethylation and reactivation of tumor suppressor genes, but it did not affect the methylation of centromeric satellite sequences. These results establish RG108 as a DNA methyltransferase inhibitor with fundamentally novel characteristics that will be particularly useful for the experimental modulation of epigenetic gene regulation.
References
Yan Shi, Caroline Desponts, Jeong Tae Do, Heung Sik Hahm, Hans R. Schöler, Sheng Ding. Induction of Pluripotent Stem Cells from Mouse Embryonic Fibroblasts by Oct4 and Klf4 with Small-Molecule Compounds. Cell Stem Cell. 2008; 3(5): 568 – 574.
Bodo Brueckner, Regine Garcia Boy, Pawel Siedlecki. Epigenetic Reactivation of Tumor Suppressor Genes by a Novel Small-Molecule Inhibitor of Human DNA Methyltransferases. Cancer Research. 2005; 65(14): 6305 – 11.
| Cell experiment: [1] | |
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Cell lines |
The human promyelocytic leukemia HL-60 cells. |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
48 h; 50 μM |
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Applications |
Cells were pretreated with 50 μM RG108 for 48 h and then after removal of the inhibitor cultivated with 1 μM RA for the next 4 days. Viable cell number was determined daily by counting in a hemocytometer after staining with 0.2% trypan blue. Cell cycle analysis of PI stained cells by flow cytometry demonstrated a slight decrease in the proportion of cells in S-phase (by 20% from control) after treatment with minor changes in G2/M. |
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References: [1] Savickiene J, Treigyte G, Borutinskaite V V, et al. Antileukemic activity of combined epigenetic agents, DNMT inhibitors zebularine and RG108 with HDAC inhibitors, against promyelocytic leukemia HL-60 cells[J]. Cellular & molecular biology letters, 2012, 17(4): 501-525. |
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| Cas No. | 48208-26-0 | SDF | |
| 别名 | N-Phthalyl-L-tryptophan,RG108 | ||
| 化学名 | (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O | ||
| 分子式 | C19H14N2O4 | 分子量 | 334.33 |
| 溶解度 | ≥ 16.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9911 mL | 14.9553 mL | 29.9106 mL |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9821 mL |
| 10 mM | 0.2991 mL | 1.4955 mL | 2.9911 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet