RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 48208-26-0
- 分子式: C19H14N2O4
- 分子量:334.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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DNA Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
CpG methylase M.SssI 115 nM (IC50) |
体外実験
RG108 (GMP) effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 (GMP) results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 (GMP) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1].
In another study, the synthesis and in vitro analysis of a biotinylated RG108 (GMP) conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2].
In a recent study, it is shown RG108 (GMP) can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 48208-26-0
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分子量 334.33
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分子式 C19H14N2O4
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SMILES
O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Brueckner B, et al. 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. [Content Brief]
[2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6. [Content Brief]
[3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RG108 (GMP) 関連分類
HY-13642G 関連分類
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