1. Epigenetics
  2. DNA Methyltransferase
  3. RG108

RG108 (Synonyms: N-Phthalyl-L-tryptophan)

Cat. No.: HY-13642 Purity: 99.75%
Handling Instructions

RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.

For research use only. We do not sell to patients.

RG108 Chemical Structure

RG108 Chemical Structure

CAS No. : 48208-26-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.

IC50 & Target

IC50: 115 nM (DNA methyltransferase)[1]

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].

Molecular Weight

334.33

Formula

C₁₉H₁₄N₂O₄

CAS No.

48208-26-0

SMILES

O=C(N1[[email protected]](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (299.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9911 mL 14.9553 mL 29.9106 mL
5 mM 0.5982 mL 2.9911 mL 5.9821 mL
10 mM 0.2991 mL 1.4955 mL 2.9911 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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.

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

References
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RG108
Cat. No.:
HY-13642
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