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质量水平
检测方案
≥98% (HPLC)
形式
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。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。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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
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
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
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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