RG108 

RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences^[1][2][3].

RG108 (GMP) effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 (GMP) results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 (GMP) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences^[1].
In another study, the synthesis and in vitro analysis of a biotinylated RG108 (GMP) conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes^[2].
In a recent study, it is shown RG108 (GMP) can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

334.33

C₁₉H₁₄N₂O₄

48208-26-0

O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.  [Content Brief]

  [2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.  [Content Brief]

  [3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.  [Content Brief]