GLPBio

RG 108

Catalog No.: GC13398Purity:>99.50%Synonyms: N-Phthalyl-L-tryptophan,RG108
COASDSData Sheet
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.

RG 108
Cas No.: 48208-26-0
10mM (in 1mL DMSO)In Stock
$47.00
1
1mgIn Stock
$12.00
1
5mgIn Stock
$27.00
1
10mgIn Stock
$43.00
1
25mgIn Stock
$88.00
1
50mgIn Stock
$148.00
1
100mgIn Stock
$236.00
1
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Description

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.

Protocol

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:
[1] 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.
[2] 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
48208-26-0
Synonyms
N-Phthalyl-L-tryptophan,RG108
Chemical Name
(2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid
SMILES
C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O
Molecular Formula
C19H14N2O4
Molecular Weight
334.33
Solubility
≥ 16.7mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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