EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72212_C
表观遗传修饰剂；抑制 DNA 甲基转移酶 (DNMT)
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总览
RG108 是一种表观遗传修饰剂，可抑制 DNA 甲基转移酶 (IC₅₀ = 115 nM)。RG108 是一种非核苷抑制剂，通过直接结合甲基转移酶，从而阻断酶的活性位点发挥作用。（Brueckner et al., Stresemann et al.）
重编程
·增强人和小鼠体细胞重编程为诱导多能干细胞 (iPS) 的效率（Mali et al., Pasha et al., Shi et al.）。
别名
N-邻苯二甲酰-L-色氨酸
细胞类型
多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
重编程
研究领域
干细胞生物学
CAS 编号
48208-26-0
化学式
C₁₉H₁₄N₂O₄
分子量
334.3 g/mol
纯度
≥98%
通路
表观遗传学
靶点
DNMT
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
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相关材料与文献
技术资料 (3)
文献 (5)
Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases.
Cancer research 2005 JUL
Abstract
DNA methylation regulates gene expression in normal and malignant cells. The possibility to reactivate epigenetically silenced genes has generated considerable interest in the development of DNA methyltransferase inhibitors. Here,we provide a detailed characterization of RG108,a novel small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of the compound resulted in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly,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.
Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines.
Cancer research 2006 MAR
Abstract
DNA methyltransferase inhibitors represent promising new drugs for cancer therapies. The first of these compounds (5-azacytidine,Vidaza) has recently been approved as an antitumor agent,and others are presently in various stages of their preclinical or clinical development. Most of the archetypal inhibitors have been established and characterized in different experimental systems,which has thus far precluded their direct comparison. We have now established defined experimental conditions that allowed a comparative analysis of the six most widely known DNA methyltransferase inhibitors: 5-azacytidine (5-aza-CR),5-aza-2'-deoxycytidine (5-aza-CdR),zebularine,procaine,(-)-epigallocatechin-3-gallate (EGCG),and RG108. Of these,5-aza-CR,5-aza-CdR,zebularine,and EGCG were found to exhibit significant cytotoxicity in human cancer cell lines. 5-aza-CdR and EGCG were also found to be genotoxic,as evidenced by the induction of micronuclei. In addition,5-aza-CR,5-aza-CdR,zebularine,and RG108 caused concentration-dependent demethylation of genomic DNA,whereas procaine and EGCG failed to induce significant effects. Finally,the experiments in cancer cell lines were complemented by a cell-free in vitro assay with purified recombinant DNA methyltransferase,which indicated that RG108 is the only drug capable of direct enzyme inhibition. These results show a substantial diversity in the molecular activities of DNA methyltransferase inhibitors and provide valuable insights into the developmental potential of individual drugs.
Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds.
Cell stem cell 2008 NOV
Abstract
Somatic cells can be induced into pluripotent stem cells (iPSCs) with a combination of four transcription factors,Oct4/Sox2/Klf4/c-Myc or Oct4/Sox2/Nanog/LIN28. This provides an enabling platform to obtain patient-specific cells for various therapeutic and research applications. However,several problems remain for this approach to be therapeutically relevant due to drawbacks associated with efficiency and viral genome integration. Recently,it was shown that neural progenitor cells (NPCs) transduced with Oct4/Klf4 can be reprogrammed into iPSCs. However,NPCs express Sox2 endogenously,possibly facilitating reprogramming in the absence of exogenous Sox2. In this study,we identified a small-molecule combination,BIX-01294 and BayK8644,that enables reprogramming of Oct4/Klf4-transduced mouse embryonic fibroblasts,which do not endogenously express the factors essential for reprogramming. This study demonstrates that small molecules identified through a phenotypic screen can compensate for viral transduction of critical factors,such as Sox2,and improve reprogramming efficiency.
更多信息
| Molecular Weight | 334.3 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | N-Phthalyl-L-Tryptophan |
| Cas Number | 48208-26-0 |
| Chemical Formula | C₁₉H₁₄N₂O₄ |
| 纯度 | ≥ 98% |
| Target | DNMT |
| Pathway | Epigenetic |
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质量保证:
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
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