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For research use only.

Catalog No.S2821

15 publications

RG108 Chemical Structure

CAS No. 48208-26-0

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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10mM (1mL in DMSO) USD 150 In stock
USD 115 In stock
USD 479 In stock
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Selleck's RG108 has been cited by 15 publications

4 Customer Reviews

  • The inhibition effect of RG108 on M.SssI MTase activity.

    Biosens Bioelectron 2015 66, 109-14. RG108 purchased from Selleck.

  • Western blot analysis of DNMT1 in fetal fibroblasts at different concentrations of RG108 (0, 10, 20, 50, 75 and 100 µM).

    Cell Physiol Biochem, 2018, 50(4):1376-1397. RG108 purchased from Selleck.

  • (A) Effect of the DNA methylation inhibitor RG108 on cell proliferation in the parental and resistant cell lines using the MTT assay.

    Oncotarget, 2015, 6(7):5134-46.. RG108 purchased from Selleck.

  • Representative IHC images showing Ki67 and CD31-staining in xenografts from Eca-109 cells (magnification, ×400).

    Oncol Rep, 2018, 39(3):993-1002. RG108 purchased from Selleck.

Purity & Quality Control

Choose Selective DNA Methyltransferase Inhibitors

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.
DNA methyltransferase [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells NYPNeGNpTnWwY4Tpc44h[XO|YYm= M3LG[|ExKM7:TR?= M2[1fVYhcA>? MWPJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZZBweHSxdHnjJINmdGy|IHH0JFExKHWPIHHmeIVzKDZiaILzJIJ6KE[LVFOtRY5v\XirbjDWM5Bzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiRlHDV{BidmGueYPpd{Bz\WyjdHn2[UB1dyClb370do9t MUOyOVgxOTF4MB?=
rat macrophages NWrMfYs4TnWwY4Tpc44h[XO|YYm= M1P5TFI1KGh? NVnJ[nl6UW6qaXLpeIlwdiCxZjDBR2FVKGmwIILheEBu[WO{b4DoZYdmeyCjc4Pld5Nm\CCjczDpcoNwenCxcnH0bY9vKG:oIHX4eJJi[2WubIXsZZIhYzOKXT3vcIVq[yCjY3nkMWJUSSClb33wcIV5KGmwdH:geIhmKGmwdILhZ4VtdHWuYYKgZ4hwdGW|dHXyfYwh\XO2ZYKgZYZ1\XJiMkSgbJJ{NCCLQ{WwQVAvPDd7IN88US=> MmLzNVk1PjRzOEm=
human HepG2 cells NHrBN2xHfW6ldHnvckBie3OjeR?= M2qzcGlvcGmkaYTpc44hd2ZiQVPBWEBqdiCqdX3hckBJ\XCJMjDj[YxteyxiSVO1NF0xNjR5OTFOwG0> NFnVUnYyQTF4N{i4PC=>
human THP1 cells MnzlSpVv[3Srb36gZZN{[Xl? NEjwenlKdmirYnn0bY9vKG:oIFHDRXQudWWmaXH0[YQh\XO2ZYLp[olm\CClaH;s[ZN1\XKxbDDhZ4N2dXWuYYTpc44hcW5iaIXtZY4hXEiSMTDj[YxteyCneIDvd4VlKHSxIHHj[ZR6dC2ORFyg[JVzcW6pIHTp[oZmemWwdHnheIlwdiCjc4Pld5Nm\CCjczDl[oZm[3Rib36g[o9idSClZXzsJIZwem2jdHnvckwhUUN3ME2xMlUh|ryP NVf6XXBOOTh4MkCzPFE>

... Click to View More Cell Line Experimental Data


Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL (200.4 mM)
Ethanol 67 mg/mL (200.4 mM)
Water 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 Information

Molecular Weight 334.33


CAS No. 48208-26-0
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O

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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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DNA Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID