RG108

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].

Product Specifications

CAS Number

[48208-26-0]

Product Name Alternative

N-Phthalyl-L-tryptophan

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

DNA Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RG108.html

Purity

99.93

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

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

Molecular Formula

C19H14N2O4

Molecular Weight

334.33

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.