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Submit ReviewRG 108 is a non-nucleoside DNA methyltransferase inhibitor that blocks the enzyme active site. Inhibits DNA methylation in human cancer cell lines in vitro without detectable toxicity. Demethylates and reactivates epigenetically silenced tumor suppressor genes. Enhances the efficiency of induced pluripotent stem cell (iPS) generation.
RG 108 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 334.33 |
公式 | C19H14N2O4 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 48208-26-0 |
PubChem ID | 702558 |
InChI Key | HPTXLHAHLXOAKV-INIZCTEOSA-N |
Smiles | O=C(C(C=CC=C4)=C4C3=O)N3[C@H](C(O)=O)CC2=CNC1=CC=CC=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 33.43 | 100 | |
ethanol | 33.43 | 100 |
以下数据基于产品分子量 334.33。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.99 mL | 14.96 mL | 29.91 mL |
5 mM | 0.6 mL | 2.99 mL | 5.98 mL |
10 mM | 0.3 mL | 1.5 mL | 2.99 mL |
50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
参考文献是支持产品生物活性的出版物。
Brueckner et al (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase. Cancer Res. 65 6305 PMID: 16024632
Stresemann et al (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794 PMID: 16510601
Schirrmacher et al (2006) Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug.Chem. 17 261 PMID: 16536454
If you know of a relevant reference for RG 108, please let us know.
关键词: RG 108, RG 108 supplier, Non-nucleoside, DNA, methyltransferase, inhibitor, inhibitors, transferases, RG108, inhibits, methylation, dnmt, epigenetics, Methyltransferases, Stem, Cell, Reprogramming, 3295, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RG 108 的部分引用包括:
Kottakis et al (2016) LKB1 loss links serine metabolism to DNA methylation and tumorigenesis. Nature 539 390 PMID: 27799657
Nugent et al (2015) Brain feminization requires active repression of masculinization via DNA methylation. PLoS One 18 690 PMID: 25821913
Zhang et al (2016) Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18 653 PMID: 27133794
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Cells are treated with 10 µM RG 108
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.