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Merck
CN

R8279

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 Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
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产品名称

RG108, ≥98% (HPLC), powder

SMILES string

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

assay

≥98% (HPLC)

form

powder

optical activity

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

color

yellow

solubility

DMSO: >10 mg/mL

storage temp.

−20°C

Quality Level

Application

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。

Biochem/physiol Actions

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。

Features and Benefits

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。

General description

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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

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