DC Chemicals Limited
China
Product Name: RG108
Price: $400.0/100mg $700.0/250mg $1300.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

48208-26-0

48208-26-0 structure

48208-26-0 structure

Name: RG108
Chemical Name: RG 108
CAS Number: 48208-26-0
Molecular Formula: C₁₉H₁₄N₂O₄
Molecular Weight: 334.326
Catalog: Biochemical Inhibitor Epigenetics DNA Methyltransferase inhibitor
Create Date: 2018-05-11 08:00:00
Modify Date: 2024-01-04 03:51:08
RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.

Name	RG 108
Synonyms	DNA Methyltransferase Inhibitor N-phthalimide l-tryptophane 1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)- N-Phthalyl-L-tryptophan (2S)-2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid N-Phth-Trp-OH RG108

Description	RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.
Related Catalog	Signaling Pathways >> Epigenetics >> DNA Methyltransferase Research Areas >> Cancer
Target	CpG methylase M.SssI:115 nM (IC50)
In Vitro	RG108 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 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 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 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2]. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].
Kinase Assay	The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains 350 to 400 ng substrate DNA and 4 units of M.SssI methylase (0.5 μM) in a final volume of 50 μL. Inhibitors are added to final concentrations of 10, 100, 200, and 500 μM, respectively. Reactions are done at 37°C for 2 hours. After completion, the reaction is inactivated at 65°C for 15 minutes and the DNA is purified using PCR Purification kit. Three hundred nanograms of purified DNA is digested for 3 hours at 60°C with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.
References	[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.

Density	1.5±0.1 g/cm3
Boiling Point	606.0±50.0 °C at 760 mmHg
Melting Point	192-194℃
Molecular Formula	C₁₉H₁₄N₂O₄
Molecular Weight	334.326
Flash Point	320.3±30.1 °C
Exact Mass	334.095367
PSA	90.47000
LogP	3.33
Appearance	yellow
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.741
Storage condition	Store at RT
Water Solubility	DMSO: >10mg/mL

RIDADR	NONH for all modes of transport