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Merck
모든 사진(1)

주요 문서

R8279

Sigma-Aldrich

RG108

≥98% (HPLC), powder

동의어(들):

N-Phthalyl-L-tryptophan

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About This Item

실험식(Hill 표기법):
C19H14N2O4
CAS Number:
Molecular Weight:
334.33
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

광학 활성

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

색상

yellow

solubility

DMSO: >10 mg/mL

저장 온도

−20°C

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

일반 설명

RG108, a non-nucleoside analog is also called [2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl) propanoic acid.

애플리케이션

RG108 has been used:
  • in reprogramming and increasing cell plasticity of primary multipotent mesenchymal stromal cells (MMSC)
  • as an inhibitor of DNA methyltransferase (DNMTi) in human retinal pigment epithelial ARPE-19 cells
  • as a DNA methyltransferase inhibitor in C33A2 cells to test its effect on papillomavirus late gene expression (HPV16)

생화학적/생리학적 작용

RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.
RG108 is less cytotoxic compared to azacytidine (5-Aza-dCR). It mediates radiosensitivity in esophageal cancer cells (EC). RG108 is a potent epigenetic modulator and a demethylating agent. It elicits non-cytotoxic functionality and may be useful in stem cell therapies based on human bone marrow-derived mesenchymal stem cells (hBMSCs). It interacts with DNA methyltransferase 1 at the catalytic domain region.

특징 및 장점

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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문서 라이브러리 방문

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
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
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
Lucia Bialesova et al.
Scientific reports, 7(1), 10152-10152 (2017-09-02)
Increased adipocyte lipolysis links obesity to insulin resistance. The lipid droplet coating-protein Perilipin participates in regulation of lipolysis and is implicated in obesity. In the present study we investigate epigenetic regulation of the PLIN1 gene by correlating PLIN1 CpG methylation

문서

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.

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