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RG 108DNA methyltransferase inhibitor

RG 108

Catalog No. A1913
Size Price Stock Qty
10mM (in 1mL DMSO) $60.00 In stock
10mg $60.00 In stock
25mg $100.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. 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

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Quality Control & MSDS

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Chemical structure

RG 108

Related Biological Data

RG 108

Related Biological Data

RG 108

Related Biological Data

RG 108

Related Biological Data

RG 108

Biological Activity

Description RG 108 is a small-molecule inhibitor of DNMT(DNA methyltransferases) with an IC50 values of 600 nM in M.SssI assay.
Targets DNMT          
IC50 600 nM          

Protocol

Cell experiment: [1]

Cell lines

The human promyelocytic leukemia HL-60 cells.

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

48 h; 50 μM

Applications

Cells were pretreated with 50 μM RG108 for 48 h and then after removal of the inhibitor cultivated with 1 μM RA for the next 4 days. Viable cell number was determined daily by counting in a hemocytometer after staining with 0.2% trypan blue. Cell cycle analysis of PI stained cells by flow cytometry demonstrated a slight decrease in the proportion of cells in S-phase (by 20% from control) after treatment with minor changes in G2/M.

Animal experiment:

Animal models

Dosage form

Applications

Other notes

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.

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Chemical Properties

Cas No. 48208-26-0 SDF Download SDF
Synonyms N-Phthalyl-L-tryptophan,RG108
Chemical Name (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid
Canonical SMILES C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O
Formula C19H14N2O4 M.Wt 334.33
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips No
Shipping Condition No

Background

RG108 is a DNA methyltransferase (DMNT) inhibitor that enhanced reprogramming of OK-transduced MEFs in the presence of BIX. It is a small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. DNA methylation regulates gene expression in normal and malignant cells. DNA methyltransferase inhibitors are able to reactivate epigenetically silenced genes. RG108 caused demethylation and reactivation of tumor suppressor genes, but it did not affect the methylation of centromeric satellite sequences. These results establish RG108 as a DNA methyltransferase inhibitor with fundamentally novel characteristics that will be particularly useful for the experimental modulation of epigenetic gene regulation.

References

Yan Shi, Caroline Desponts, Jeong Tae Do, Heung Sik Hahm, Hans R. Schöler, 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.

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.