RG 108
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
RG108是一种DNA甲基转移酶(DMNT)抑制剂,可以增强BIX存在条件下OK转导的MEFs的重编程。RG108是一种小分子,在体外实验中可以有效阻断DNA甲基转移酶,但不会引起人源细胞系中共价酶的俘获。DNA甲基化具有调控正常以及癌变细胞中基因表达的作用。DNA甲基转移酶(DMNT)抑制剂能够重新激活表观沉默基因。RG108能够引起去甲基化并且重新激活肿瘤抑制基因,但是不会影响着丝粒卫星DNA序列的甲基化。上述结果足以证明RG108是一种具有全新特性的DNA甲基转移酶(DMNT)抑制剂,在表观遗传学基因调控的实验调制中将会尤其有效。
参考文献:
[1] Yan Shi, Caroline Desponts, Jeong Tae Do, Heung Sik Hahm, Hans R. Schler, Sheng Ding. Induction of Pluripotent Stem Cells from Mouse Embryonic Fibroblasts by Oct4 and Klf4 with Small-Molecule Compounds. Cell Stem Cell. 2008; 3(5): 568 – 574.
[2] Bodo Brueckner, Regine Garcia Boy, Pawel Siedlecki. Epigenetic Reactivation of Tumor Suppressor Genes by a Novel Small-Molecule Inhibitor of Human DNA Methyltransferases. Cancer Research. 2005; 65(14): 6305 – 11.
- 1.Zhang B, Wang W, et al. "Inositol polyphosphate-4-phosphatase type II plays critical roles in the modulation of cadherin-mediated adhesion dynamics of pancreatic ductal adenocarcinomas." Cell Adh Migr. 2018 Aug 19:1-16. PMID:29952716
- 2.Stenzig J, Schneeberger Y, et al. "Pharmacological inhibition of DNA methylation attenuates pressure overload-induced cardiac hypertrophy in rats." J Mol Cell Cardiol. 2018 May 21;120:53-63. PMID:29792884
- 3.Schneeberger, Yvonne, et al. "Pharmacokinetics of the Experimental Non‐Nucleosidic DNA Methyl Transferase Inhibitor N‐Phthalyl‐L‐Tryptophan (RG 108) in Rats." Basic & clinical pharmacology & toxicology (2015). PMID:26525153
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 334.33 |
Cas No. | 48208-26-0 |
Formula | C19H14N2O4 |
Synonyms | N-Phthalyl-L-tryptophan,RG108 |
Solubility | insoluble in H2O; ≥16.7 mg/mL in DMSO; ≥45.9 mg/mL in EtOH |
Chemical Name | (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
人类早幼粒细胞白血病HL-60细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
48 h;50 μM |
实验结果 |
使用50 μM的RG108预处理细胞48小时,然后除去抑制剂,接下来用1 μM RA培养4天。使用0.2%的台盼蓝染色,随后用血细胞计数器测定活细胞数目。通过流式细胞术分析PI染色细胞的细胞周期,结果表明,G2/M具有微小变化,S期细胞比例略有降低,比对照中减少20%。 |
References: [1] Savickiene J, Treigyte G, Borutinskaite V V, et al. Antileukemic activity of combined epigenetic agents, DNMT inhibitors zebularine and RG108 with HDAC inhibitors, against promyelocytic leukemia HL-60 cells[J]. Cellular & molecular biology letters, 2012, 17(4): 501-525. |
Description | RG 108是一种小分子DNMT(DNA甲基转移酶) 抑制剂,在M.SssI 试验中的IC50值为600 nM。 | |||||
靶点 | DNMT | |||||
IC50 | 600 nM |
质量控制和MSDS
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