RG108

Catalog No.S2821 Synonyms: N-Phthalyl-L-tryptophan

For research use only.

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

RG108 Chemical Structure

CAS No. 48208-26-0

Selleck's RG108 has been cited by 18 publications

Purity & Quality Control

Choose Selective DNA Methyltransferase Inhibitors

Biological Activity

Description RG108 (N-Phthalyl-L-tryptophan) 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)
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 THP1 cells M3TYcmZ2dmO2aX;uJIF{e2G7 NUPub3lqUW6qaXLpeIlwdiCxZjDBR2FVNW2nZHnheIVlKGW|dHXybYZq\WRiY3jvcIV{fGW{b3ygZYNkfW23bHH0bY9vKGmwIHj1cYFvKFSKUEGgZ4VtdHNiZYjwc5Nm\CC2bzDhZ4V1gWxvTFTMJIR2emmwZzDkbYZn\XKnboTpZZRqd25iYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJIZw[W1iY3XscEBnd3KvYYTpc44tKEmFNUC9NU42KM7:TR?= NVWye2tIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2NlA{QDFpPkG4OlIxOzhzPD;hQi=>
human HepG2 cells M3P6c2Z2dmO2aX;uJIF{e2G7 MlX0TY5pcWKrdHnvckBw\iCDQ1HUJIlvKGi3bXHuJGhmeEd{IHPlcIx{NCCLQ{WwQVAvPDd7IN88US=> NHXXb5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG2O|g5QCd-MUmxOlc5QDh:L3G+
rat macrophages NFvNeoxHfW6ldHnvckBie3OjeR?= M3XQ[FI1KGh? MV\Jcohq[mm2aX;uJI9nKEGFQWSgbY4hemG2IH3hZ5JweGijZ3XzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4Yh\Xi2cnHj[YxtfWyjcjDbN2heNW:uZXnjJIFkcWRvQmPBJINwdXCuZYigbY51dyC2aHWgbY51emGlZXzseYxieiClaH;s[ZN1\XK7bDDld5RmeiCjZoTldkAzPCCqcoOsJGlEPTB;MD60O|kh|ryP M4D0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NE[0NVg6Lz5zOUS2OFE5QTxxYU6=
MCF7 MnzERZBweHSxc3nzJIF{e2G7 NUD0XolSOTBidV2= M4DlOVYhcHK| NHPnWnJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[XCxcITveIlkKGOnbHzzJIF1KDFyIIXNJIFnfGW{IE[gbJJ{KGK7IF\JWGMuSW6wZYjpckBXN3C{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSgSmFEWyCjbnHsfZNqeyC{ZXzheIl3\SC2bzDjc451em:u M33WSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OECxNVYxLz5{NUiwNVE3ODxxYU6=
MCF7 NHn5[nJCeG:ydH;zbZMh[XO|YYm= NHzTT44yOCC3TR?= NYHBdnBsPiCqcoO= MojRTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRm[WRiY3XscJMh[XRiMUCgeW0h[W[2ZYKgOkBpenNiYomgSmlVSy2Dbn7lfIlvKFZxcILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBHSUOVIHHuZYx6e2m|IILlcIF1cX[nIITvJINwdnS{b3y= NFjCVmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwNVE3OCd-MkW4NFEyPjB:L3G+
MCF7 MWHGeY5kfGmxbjDhd5NigQ>? NYfwdVViOTByIIXN MWKxJIhz M{PyZWNwdXCndHn0bZZmKGmwaHnibZRqd25ib3[gSG5OXDFiaX6gLHMqNU2ndHj5cEAzNSh{LEWt[IlwgG9vMjy1MYRqcHmmcn:tNWgueHm{cn;sMVEugWxrLUOtLFUuMHC{b4CtNk16di1zLYnsc5h6MS1zSD3pcoRwdC1|LYnsLZBzd3Cjbn;heIUhdGGkZXzl[EBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFyMDD1UUBxemWrbnP1ZoF1\WRiZn;yJFEhcHJiZn;scI94\WRiYomgZ4VtdCCuYXLlcIlv\yCob4KgN|AhdWmwczDhcoQh[2yrY3vl[EB4cXSqIGTFVk1RTQ>? NFj4W2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwNVE3OCd-MkW4NFEyPjB:L3G+
MCF7 NGnKW2hHfW6ldHnvckBie3OjeR?= MnLmOVAhfG9iNUCwJJVO MXKxJIhz MmPFR49ueGW2aYTpeoUhcW6qaXLpeIlwdiCxZjDEUm1VOSCrbjCoV{kuVWW2aInsJFIuMDJuNT3kbY95dy1{LEWt[IlpgWS{bz2xTE1xgXK{b3ytNU16dClvMz2oOU0peHKxcD2yMZlvNTFveXzvfJkqNTGKLXnu[I9tNTNveXypdJJweGGwb3H0[UBt[WKnbHXkJIh2dWGwIF3DSlch[2WubIOgZZQhPTBidH:gOVAxKHWPIIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSClZXzsJIxi[mWuaX7nJIZweiBzIHjyJIFv\CClbHnjb4VlKHerdHigWGVT NHLXNZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwNVE3OCd-MkW4NFEyPjB:L3G+
SK-N-MC MmjjdWhVWyCjc4PhfS=> MkTDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

Protocol (from 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 Research:[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.

Solubility (25°C)

In vitro

DMSO 67 mg/mL
(200.4 mM)
Water Insoluble
Ethanol '67 mg/mL

Chemical Information

Molecular Weight 334.33
Formula

C19H14N2O4

CAS No. 48208-26-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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.

Handling Instructions

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