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Merck
CN

R8279

Sigma-Aldrich

RG108

≥98% (HPLC), DNA methyltransferase (DMNT) inhibitor, powder

别名:

N-酞酰-L-色氨酸

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关于此项目

经验公式(希尔记法):
C19H14N2O4
化学文摘社编号:
分子量:
334.33
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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产品名称

RG108, ≥98% (HPLC), powder

质量水平

方案

≥98% (HPLC)

表单

powder

旋光性

[α]/D -250 to -310°, c = 0.5 in methanol

颜色

yellow

溶解性

DMSO: >10 mg/mL

储存温度

−20°C

SMILES字符串

OC(=O)[C@H](Cc1c[nH]c2ccccc12)N3C(=O)C4=CCCC=C4C3=O

InChI

1S/C19H16N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h3-8,10,16,20H,1-2,9H2,(H,24,25)/t16-/m0/s1

InChI key

LMAZUAXDZRILNJ-INIZCTEOSA-N

一般描述

RG108是一种非核苷类似物,也称为[2-(1,3-二氧异吲哚啉-2-基)-3-(1H-吲哚-3-基)丙酸。

应用

RG108可用于:
  • 重编程和提高原代多能间充质干细胞 (MMSC) 的可塑性。
  • 作为人视网膜色素上皮细胞ARPE-19中的DNA甲基转移酶抑制剂 (DNMTi)。
  • 作为C33A2细胞的DNA甲基转移酶抑制剂,检测其对乳头瘤病毒晚期基因表达 (HPV16) 的影响。

生化/生理作用

RG108是一种DNA甲基转移酶(DMNT)抑制剂。
RG108是一种DNA甲基转移酶(DMNT)抑制剂。它通过DNA去甲基化重新激活肿瘤细胞中的肿瘤抑制基因表达(p16,SFRP1,分泌性卷曲相关蛋白-1和TIMP-3)。RG108还能抑制人肿瘤细胞系(HCT116,NALM-6)增殖并增加培养的倍增时间。
Rg108的细胞毒性低于氮杂胞苷 (5-Aza-dCR)。它介导食道癌细胞 (EC) 的辐射敏感性。RG108是有效的表观遗传调控剂和去甲基化剂。它不会引起细胞毒性,可用于基于人骨髓间充质干细胞 (hBMSC) 的干细胞治疗。它作用于DNA甲基转移酶1的催化结构域。

特点和优势

这种化合物是基因调控研究的特色产品。点击此处发现更多特色基因调控产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

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Peter Karagiannis et al.
Physiological reviews, 99(1), 79-114 (2018-10-18)
The discovery of somatic cell nuclear transfer proved that somatic cells can carry the same genetic code as the zygote, and that activating parts of this code are sufficient to reprogram the cell to an early developmental state. The discovery
Paulina Tokarz et al.
European journal of pharmacology, 776, 167-175 (2016-02-24)
Epigenetic modifications influence DNA damage response (DDR). In this study we explored the role of DNA methylation and histone acetylation in DDR in cells challenged with acute or chronic oxidative stress. We used retinal pigment epithelial cells (ARPE-19), which natively
Yao Ou et al.
Oncology reports, 39(3), 993-1002 (2018-01-13)
Esophageal cancer (EC) is the eighth most common highly aggressive cancer worldwide. The purpose of this study was to investigate the effect of the DNA methyltransferase inhibitor RG108 on the radiosensitivity of EC cells. MTT and clonogenic assays were performed
Qing Wang et al.
Journal of cellular biochemistry, 119(2), 1501-1510 (2017-08-05)
DNA methylation plays a crucial role in lots of biological processes and cancer. 5-azacytidine (5-AC), a DNA methylation inhibitor, has been used as a potential chemotherapeutic agent for cancer. In this study, we used 5-AC treatment to investigate whether DNA
German Todorov et al.
Scientific reports, 9(1), 8741-8741 (2019-06-21)
Mental health disorders are manifested in families, yet cannot be fully explained by classical Mendelian genetics. Changes in gene expression via epigenetics present a plausible mechanism. Anxiety often leads to avoidant behaviors which upon repetition may become habitual, maladaptive and

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