RG 108 (Synonyms: N-Phthalyl-L-tryptophan,RG108) |
Catalog No.GC13398
One-Click Copy Product Info
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RG 108 is a potent DNA methyltransferase inhibitor, with an IC50 value of 115nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 48208-26-0
Sample solution is provided at 25 µL, 10mM.
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RG 108 is a potent DNA methyltransferase inhibitor, with an IC50 value of 115nM[1]. By targeting DNA methyltransferases, RG 108 significantly reduced the hypermethylation levels of GSTP1, APC, and RAR-β2 promoters in prostate cancer cells, affecting cell cycle progression[2]. RG 108 has been widely used to increase the reprogramming efficiency of induced pluripotent stem cells (iPSCs) and improve blastocyst formation[3].
In vitro, RG 108 treatment for 12h significantly inhibited the proliferation of Eca-109 and TE-1 cells with IC50 values of 70µM and 75µM, respectively[4]. Treatment with 50μM RG 108 for 3 days increased the expression of NANOG, OCT4, and CD105 in human bone marrow mesenchymal stem cells (hBMSCs), accompanied by a significant reduction in the transcriptional levels of DNMTs[5]. Treatment with 100μM RG 108 for 5 days reversed the senescence phenotype of human periodontal ligament stem cells (hPDLSCs) and stimulated adipogenesis of pPDLSCs[6].
In vivo, RG 108 treatment via intraperitoneal injection at a dose of 20mg/kg/day for 3 days significantly attenuated cisplatin-induced acute kidney injury in mice, resulting in reduced tubular dilatation and glycogen deposition[7]. A single dose of RG 108 (10mg/kg) injected intraperitoneally 2 hours before noise exposure can improve noise-induced hearing loss, reduce hair cell damage, and auditory synapse loss in mice[8].
References:
[1] Brueckner B, Garcia Boy R, Siedlecki P, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases[J]. Cancer research, 2005, 65(14): 6305-6311.
[2] Graça I, J. Sousa E, Baptista T, et al. Anti-tumoral effect of the non-nucleoside DNMT inhibitor RG108 in human prostate cancer cells[J]. Current pharmaceutical design, 2014, 20(11): 1803-1811.
[3] Wu C, Zhang D, Zhang S, et al. Optimizing treatment of DNA methyltransferase inhibitor RG108 on porcine fibroblasts for somatic cell nuclear transfer[J]. Reproduction in Domestic Animals, 2019, 54(12): 1604-1611.
[4] Ou Y, Zhang Q, Tang Y, et al. DNA methylation enzyme inhibitor RG108 suppresses the radioresistance of esophageal cancer[J]. Oncology Reports, 2018, 39(3): 993-1002.
[5] Assis R I F, Wiench M, Silverio K G, et al. RG108 increases NANOG and OCT4 in bone marrow-derived mesenchymal cells through global changes in DNA modifications and epigenetic activation[J]. PLoS One, 2018, 13(12): e0207873.
[6] Roato I, Baima G, Orrico C, et al. Senescent markers expressed by periodontal ligament-derived stem cells (PDLSCs) harvested from patients with periodontitis can Be rejuvenated by RG108[J]. Biomedicines, 2023, 11(9): 2535.
[7] Kong F, Liu H, Xu T, et al. RG108 attenuates acute kidney injury by inhibiting P38 MAPK/FOS and JNK/JUN pathways[J]. International Immunopharmacology, 2024, 142: 113077.
[8] Zheng Z, Zeng S, Liu C, et al. The DNA methylation inhibitor RG108 protects against noise-induced hearing loss[J]. Cell Biology and Toxicology, 2021, 37(5): 751-771.
| Cell experiment [1]: | |
Cell lines | Eca-109 cells |
Preparation Method | Eca-109 cells were cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 100µg/ml streptomycin and 100U/ml penicillin in a humidified incubator at 37℃ with 5% CO2. Cells were seeded in 96-well flat-bottom plates at a density of 2.5×103 cells/well and treated with different concentrations of RG 108 (5, 10, 25, 50, 75, 100, 150, and 200µM) for 24 hours. 20μl of MTT solution at a concentration of 5mg/ml was added to each well, and the culture was continued for 4 hours, and the absorbance was measured at a wavelength of 490nm by the tester. |
Reaction Conditions | 5, 10, 25, 50, 75, 100, 150, and 200µM; 24h |
Applications | RG 108 treatment inhibited the cell viability of Eca-109 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Male C57BL/6J mice were maintained in a standard sterile environment with ad libitum access to diet and water. Thirty-six male C57BL/6J mice (20-22g) were randomly divided into four groups: saline control group, drug group, cisplatin induction group, and RG 108 treatment group. In the drug group, RG 108 (20mg/kg) was injected intraperitoneally. In the cisplatin-induced group, mice were intraperitoneally injected with cisplatin (20mg/kg). In the RG 108-treated group, RG 108 at a concentration of 20mg/kg was injected intraperitoneally once daily for three days. Mice were anesthetized with 5% isoflurane, and the kidneys were removed for analysis. |
Dosage form | 20mg/kg/day for 3 days; i.p. |
Applications | RG 108 treatment significantly attenuated cisplatin-induced acute kidney injury in mice. |
References: | |
| Cas No. | 48208-26-0 | SDF | |
| Synonyms | N-Phthalyl-L-tryptophan,RG108 | ||
| Chemical Name | (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O | ||
| Formula | C19H14N2O4 | M.Wt | 334.33 |
| Solubility | ≥ 16.7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9911 mL | 14.9553 mL | 29.9106 mL |
| 5 mM | 598.2 μL | 2.9911 mL | 5.9821 mL |
| 10 mM | 299.1 μL | 1.4955 mL | 2.9911 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)