RG108
Based on 14 publication(s) in Google Scholar
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 48208-26-0
- Formula: C19H14N2O4
- Molecular Weight:334.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RG108
More- Biomaterials. 2026 Jan:324:123544. [Abstract]
- Cancer Lett. 2025 Aug 29:633:218010. [Abstract]
- Genome Biol. 2025 Jul 11;26(1):202. [Abstract]
- Anal Chem. 2026 Jun 30;98(25):19187-19197. [Abstract]
- J Funct Biomater. 2026 May 8;17(5):236. [Abstract]
- Life Sci. 2020 Jan 15;241:117103. [Abstract]
- Antiviral Res. 2020 Nov;183:104931. [Abstract]
- Proc Biol Sci. 2023 Dec 6;290(2012):20232093. [Abstract]
- Int J Food Sci Tech. 2024 Jul 18.
- Funct Integr Genomics. 2024 Jan 17;24(1):12. [Abstract]
- Biochem Biophys Res Commun. 2025 Jun 16:776:152214. [Abstract]
- Respir Physiol Neurobiol. 2023 Jul:313:104060. [Abstract]
- bioRxiv. 2023 Feb 16.
- Patent. US20180263995A1.
Customer Validation & Images
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IF
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RT-PCR
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In Vivo Efficacy Study
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RT-PCR
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IF
All DNA Methyltransferase Isoforms
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Biological Activity
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CpG methylase M.SssI 115 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>200 μM
Compound: RG-108
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Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay
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[PMID: 38823264] |
| HeLa | IC50 |
>200 μM
Compound: RG-108
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Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
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[PMID: 38823264] |
| K562 | IC50 |
>200 μM
Compound: RG-108
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Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
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[PMID: 38823264] |
| MCF7 | GI50 |
127.9 μM
Compound: RG108
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Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay
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[PMID: 25801160] |
| Sf9 | IC50 |
315 μM
Compound: 11, RG-108
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Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid
Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid
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[PMID: 25406944] |
| Sf9 | IC50 |
390 μM
Compound: 11, RG-108
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Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
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[PMID: 25406944] |
| SiHa | IC50 |
>200 μM
Compound: RG-108
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Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay
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[PMID: 38823264] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 48208-26-0
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Appearance Solid
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Molecular Weight 334.33
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Formula C19H14N2O4
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Color Light yellow to yellow
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SMILES
O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O
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Synonyms
N-Phthalyl-L-tryptophan
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Biomaterials
Disrupting tumor homeostasis with an autoamplificatory nanoinducer to augment pyroptosis for efficient immunotherapy. [Abstract]2026 Jan:324:123544. PMID: 40652803 -
Cancer Lett
Targeting MKK3/c-Myc interaction to overcome osimertinib acquired resistance in EGFR mutant lung cancer. [Abstract]2025 Aug 29:633:218010. PMID: 40886822 -
Genome Biol
2025 Jul 11;26(1):202. PMID: 40646558
RG108 purchased from MedChemExpress. Usage Cited in: Genome Biol. 2025 Jul 11;26(1):202. [Abstract]
Detection of methylation levels by immunofluorescence (IF) in cells treated with 5-aza-dC or RG108 (150 μM, 3 h).
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Anal Chem
Ultrasensitive Detection of Active Turnover of DNA Methylation Using Single-Molecule Arrays with Clinical Implications. [Abstract]2026 Jun 30;98(25):19187-19197. PMID: 42275535 -
J Funct Biomater
Direct Chemical Reprogramming of Human Fibroblasts into Retinal Progenitor-like Cells for Ocular Delivery. [Abstract]2026 May 8;17(5):236. PMID: 42188405 -
Life Sci
2020 Jan 15;241:117103. PMID: 31783053 -
Antiviral Res
Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: Efficacy of decitabine and valganciclovir alone or in combination. [Abstract]2020 Nov;183:104931. PMID: 32926887 -
Proc Biol Sci
2023 Dec 6;290(2012):20232093. PMID: 38052245
RG108 purchased from MedChemExpress. Usage Cited in: Proc Biol Sci. 2023 Dec 6;290(2012):20232093. [Abstract]
A single topical application of RG108 (2 μL of 0.2 mM diluted in DMSO) on the thorax increased mean survival of B. terrestris workers by 43%.
RG108 purchased from MedChemExpress. Usage Cited in: Proc Biol Sci. 2023 Dec 6;290(2012):20232093. [Abstract]
sirt1 was significantly overexpressed in treatment workers one week after treatment with RG108 （a single topical application on the thorax，2 μL of 0.2 mM diluted in DMSO）.
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RG108 purchased from MedChemExpress. Usage Cited in: Int J Food Sci Tech. 2024 Jul 18.
RG108 (10 μM, 12 h) mitigated betaine-induced decrease in Keap1 mRNA levels in L02 cells.
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Funct Integr Genomics
DNMT1/DNMT3a-mediated promoter hypermethylation and transcription activation of ICAM5 augments thyroid carcinoma progression. [Abstract]2024 Jan 17;24(1):12. PMID: 38228798 -
Biochem Biophys Res Commun
ZBTB12 promotes breast cancer progression through transcriptional activation of the DNMT3B/ALDH1A2 axis. [Abstract]2025 Jun 16:776:152214. PMID: 40543226 -
Respir Physiol Neurobiol
2023 Jul:313:104060. PMID: 37031925 -
RG108 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 16.
RG108 significantly reduces the overall methylation level of the genome in human SK-Hep-1 cells (Fig E and G).
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Solvent & Solubility
DMSO : 100 mg/mL (299.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 1 mg/mL (2.99 mM); Clear solution; Need ultrasonic and warming and heat to 70°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9911 mL | 14.9553 mL | 29.9106 mL | 74.7764 mL |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9821 mL | 14.9553 mL | |
| 10 mM | 0.2991 mL | 1.4955 mL | 2.9911 mL | 7.4776 mL | |
| 15 mM | 0.1994 mL | 0.9970 mL | 1.9940 mL | 4.9851 mL | |
| 20 mM | 0.1496 mL | 0.7478 mL | 1.4955 mL | 3.7388 mL | |
| 25 mM | 0.1196 mL | 0.5982 mL | 1.1964 mL | 2.9911 mL | |
| 30 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4925 mL | |
| 40 mM | 0.0748 mL | 0.3739 mL | 0.7478 mL | 1.8694 mL | |
| 50 mM | 0.0598 mL | 0.2991 mL | 0.5982 mL | 1.4955 mL | |
| 60 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 80 mM | 0.0374 mL | 0.1869 mL | 0.3739 mL | 0.9347 mL | |
| 100 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL |
RG108 Related Classifications
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