Art. -Nr.: HY-13642

RG108

(Synonyms: N-Phthalyl-L-tryptophan)

14 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.93%
CAS. Nr.: 48208-26-0
Formel: C₁₉H₁₄N₂O₄
Molecular Weight:334.33

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RG108 Chemical Structure

CAS. Nr.: 48208-26-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CpG methylase M.SssI

115 nM (IC₅₀)

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	>200 μM Compound: RG-108	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	[PMID: 38823264]
HeLa	IC₅₀	>200 μM Compound: RG-108	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	[PMID: 38823264]
K562	IC₅₀	>200 μM Compound: RG-108	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	[PMID: 38823264]
MCF7	GI₅₀	127.9 μM Compound: RG108	Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay	[PMID: 25801160]
Sf9	IC₅₀	315 μM Compound: 11, RG-108	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	[PMID: 25406944]
Sf9	IC₅₀	390 μM Compound: 11, RG-108	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	[PMID: 25406944]
SiHa	IC₅₀	>200 μM Compound: RG-108	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	[PMID: 38823264]

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].

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

Chemical Information

CAS. Nr. 48208-26-0
Appearance Solid
Molecular Weight 334.33
Formel C₁₉H₁₄N₂O₄
Color Light yellow to yellow
SMILES

O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O
Synonyms

N-Phthalyl-L-tryptophan
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All IFIn Vivo Efficacy StudyRT-PCR

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Journal Impact Factor

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

DNA 5mC methylation inhibits the formation of G-quadruplex structures in the genome. [Abstract]

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).
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

Epigenetic modulation of glycoprotein VI gene expression by DNA methylation. [Abstract]

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

DNA methylation extends lifespan in the bumblebee Bombus terrestris. [Abstract]

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）.
Int J Food Sci Tech

2024 Jul 18.

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.
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

Effects of DNA Methylase Inhibitors in a Murine Model of Severe BPD. [Abstract]

2023 Jul:313:104060. PMID: 37031925
bioRxiv

2023 Feb 16.

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).
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

RG108

14 Cited Publications

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RG108

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Peptidomimetic Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RG108

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RG108

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Peptidomimetic Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RG108

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RG108 Related Classifications

HY-13642 Related Classifications