RG 108
(Synonyms: N-Phthalyl-L-tryptophan,RG108) 目录号 : GC13398
RG 108是一种强效的DNA甲基转移酶抑制剂，IC50值为115nM。
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.
RG 108是一种强效的DNA甲基转移酶抑制剂，IC50值为115nM[1]。通过靶向DNA甲基转移酶，RG 108显著降低了前列腺癌细胞中GSTP1、APC和RAR-β2启动子的高甲基化水平，从而影响细胞周期进程[2]。RG 108已广泛用于提高诱导多能干细胞（iPSCs）的重编程效率和改善囊胚形成[3]。
在体外，RG 108处理12小时显著抑制了Eca-109和TE-1细胞的增殖，IC50值分别为70µM和75µM[4]。用50μM的RG 108处理3天增加了人骨髓间充质干细胞（hBMSCs）中NANOG、OCT4和CD105的表达，同时伴随着DNMTs转录水平的显著降低[5]。用100μM的RG 108处理5天逆转了人牙周膜干细胞（hPDLSCs）的衰老表型，并刺激了hPDLSC的脂肪形成[6]。
在体内，以20mg/kg/day的剂量腹腔注射RG 108连续3天显著减轻了顺铂诱导的小鼠急性肾损伤，导致肾小管扩张和糖原沉积减少[7]。在噪声暴露前2小时单次腹腔注射RG 108（10mg/kg）可改善噪声诱导的小鼠听力损失，减少毛细胞损伤和听觉突触丢失[8]。
| 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 | |
| 别名 | N-Phthalyl-L-tryptophan,RG108 | ||
| 化学名 | (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 | ||
| 分子式 | C19H14N2O4 | 分子量 | 334.33 |
| 溶解度 | ≥ 16.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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