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重要文件

R8279

Sigma-Aldrich

RG108

≥98% (HPLC), powder

同義詞:

N-酞酰-L-色氨酸

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About This Item

經驗公式(希爾表示法):
C19H14N2O4
CAS號碼:
分子量::
334.33
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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品質等級

化驗

≥98% (HPLC)

形狀

powder

光學活性

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

顏色

yellow

溶解度

DMSO: >10 mg/mL

儲存溫度

−20°C

SMILES 字串

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 密鑰

LMAZUAXDZRILNJ-INIZCTEOSA-N

一般說明

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

應用

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。[3]
  • 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)。[4]
  • 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。[5]

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。[1]RG108是有效的表观遗传调控剂和去甲基化剂。[2]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。[2]它作用于DNA甲基转移酶1的催化结构域。[4]

特點和優勢

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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
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
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
Cecilia Johansson et al.
Virology, 482, 244-259 (2015-04-23)
We report that many histone modifications are unevenly distributed over the HPV16 genome in cervical cancer cells as well as in HPV16-immortalized keratinocytes. For example, H3K36me3 and H3K9Ac that are common in highly expressed cellular genes and over exons, were
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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We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

我們提供各種小分子研究工具,例如轉錄因子調節劑、染色質修飾酵素的抑制劑,以及用於基因調控研究中靶點鑑定和驗證的激效劑/拮抗劑;以下是這些研究工具的精選。

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