RG108

Catalog No.S2821

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

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RG108 Chemical Structure

RG108 Chemical Structure
Molecular Weight: 334.33

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Product Description

Biological Activity

Description RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.
Targets DNA methyltransferase [1]
(Cell-free assay)
IC50 115 nM
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]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro methylation 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.

Cell Assay: [1]

Cell lines HCT116 cells
Concentrations 1-100 μM
Incubation Time 5 days
Method For the determination of cellular growth and viability, cells are stained with trypan blue and counted using a standard counting grid.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Brueckner B, et al, Cancer Res, 2005, 65(14), 6305-6311.

[2] Schirrmacher E, et al, Bioconjug Chem, 2006, 17(2), 261-266.

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Chemical Information

Download RG108 SDF
Molecular Weight (MW) 334.33
Formula

C19H14N2O4

CAS No. 48208-26-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 67 mg/mL (200.4 mM)
Ethanol 67 mg/mL (200.4 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-

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Source Biosens Bioelectron 2015 66, 109-14. RG108 purchased from Selleck
Method M.SssI MTase activity
Cell Lines
Concentrations 0-1000 nM
Incubation Time 2 h
Results Therefore, to further testifies the application ability of the developed method for DNA MTase inhibitor screening, the influence of RG108 (a kind of DNA MTase inhibitor) on M.SssI MTase activity was investigated. RG108 is a novel small molecule that effectively blocked DNA methyltransferases in vitro and did not cause covalent enzyme trapping in human cell lines. As shown in Figure, the inhibition percentage increased with increasing RG108 concentration, and the maximum inhibition was achieved to 87.02%. From Figure, the IC50 value of RG108 for M.SssI MTase was calculated to be 152.54 nM, which was closed to prior report of 115.2 nM, and the small distinction may be caused by different detection methods. These results demonstrated that the proposed method presented potential in analyzing the inhibition effects of anticancer drugs on DNA MTase activity and screening DNA MTase inhibitors.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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