RG108
- Product Name
- RG108
- CAS No.
- 48208-26-0
- Chemical Name
- RG108
- Synonyms
- 108;R 108;CS-1518;RG108 >98%;RG108/RG-108;RG108 USP/EP/BP;RG108, 10 mM in DMSO;N-Phthalyl-L-tryptophan;N-Phthaloyl-L-tryptophan;N-Phthalyl-L-tryptophan>
- CBNumber
- CB0972112
- Molecular Formula
- C19H14N2O4
- Formula Weight
- 334.33
- MOL File
- 48208-26-0.mol
RG108 Property
- Melting point:
- 192-194℃
- Boiling point:
- 606.0±50.0 °C(Predicted)
- Density
- 1.502±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- DMSO: >10mg/mL
- pka
- 3.62±0.10(Predicted)
- form
- powder
- color
- yellow
- optical activity
- [α]/D -250 to -310°, c =0.5 in methanol
- Sensitive
- Light Sensitive
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
- CAS DataBase Reference
- 48208-26-0
Safety
- WGK Germany
- 3
- HS Code
- 2933.99.9701
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- R8279
- Product name
- RG108
- Purity
- ≥98% (HPLC), powder
- Packaging
- 10mg
- Price
- $278.35
- Updated
- 2025/07/31
- Product number
- P2023
- Product name
- N-Phthalyl-L-tryptophan
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 50mg
- Price
- $138
- Updated
- 2025/07/31
- Product number
- P2023
- Product name
- N-Phthalyl-L-tryptophan
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 200mg
- Price
- $409
- Updated
- 2025/07/31
- Product number
- 13302
- Product name
- RG-108
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 13302
- Product name
- RG-108
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $115
- Updated
- 2024/03/01
RG108 Chemical Properties,Usage,Production
Description
RG-108 (48208-26-0) is a non-nucleoside DNA methyltransferase inhibitor. IC50=115 nM1 Inhibits DNA methylation in human tumor cell lines without toxicity2. RG-108 enhances the reversion of neural progenitor cells to the pluripotent state.3
Uses
DNA methylation regulates gene expression in normal and malignant cells. RG-108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro). It significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like 5-azacytidine. Further, RG-108 inhibits DNA methyltransferase activity by blocking the enzyme active site. Through these actions, RG-108 demethylates and reactivates epigenetically silenced tumor suppressor genes.
Uses
RG108 has been used:
- in reprogramming and increasing cell plasticity of primary multipotent mesenchymal stromal cells (MMSC)
- as an inhibitor of DNA methyltransferase (DNMTi) in human retinal pigment epithelial ARPE-19 cells
- as a DNA methyltransferase inhibitor in C33A2 cells to test its effect on papillomavirus late gene expression (HPV16)
Definition
ChEBI: (2S)-2-(1,3-dioxo-2-isoindolyl)-3-(1H-indol-3-yl)propanoic acid is an indolyl carboxylic acid.
General Description
RG108, a non-nucleoside analog is also called [2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl) propanoic acid.
Biological Activity
Non-nucleoside DNA methyltransferase inhibitor that blocks the enzyme active site. Inhibits DNA methylation in human cancer cell lines in vitro without detectable toxicity. Demethylates and reactivates epigenetically silenced tumor suppressor genes.
Biochem/physiol Actions
RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.
Synthesis
73-22-3
438470-19-0
32675-71-1
The general procedure for the synthesis of milnacipran from L-tryptophan and 2,5-dioxopyrrolidin-1-methyl phthalate is as follows: the reaction of RG108 with L-tryptophan was carried out in a mixed solvent of water/acetonitrile under alkaline conditions (Na2CO3). After completion of the reaction, the reaction mixture was acidified with 2N HCl and subsequently extracted with ethyl acetate. The extract was evaporated to remove the solvent and the target product was obtained in 100% yield. The resulting pure yellow powder was analyzed by mass spectrometry (ESI) and 1H- and 13C-NMR for structural confirmation.
storage
Room temperature
References
[1] BODO BRUECKNER. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases.[J]. Cancer research, 2005, 65 14: 6305-6311. DOI:10.1158/0008-5472.can-04-2957
[2] CARLO STRESEMANN. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines.[J]. Cancer research, 2006, 66 5: 2794-2800. DOI:10.1158/0008-5472.can-05-2821
[3] ILONA SZABLOWSKA-GADOMSKA. Treatment with small molecules is an important milestone towards the induction of pluripotency in neural stem cells derived from human cord blood.[J]. Acta neurobiologiae experimentalis, 2012, 72 4: 337-350. DOI:10.55782/ane-2012-1906
RG108 Preparation Products And Raw materials
Raw materials
Preparation Products
RG108 Suppliers
- Tel
- 18210857532; 18210857532
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15838
- Advantage
- 69
- Tel
- 021-67121386
- Fax
- 021-67121385
- Sales-CN@TCIchemicals.com
- Country
- China
- ProdList
- 24529
- Advantage
- 81
- Tel
- 0330-2528181
- Fax
- 0330-2528171
- sales@vdmbio.com
- Country
- United States
- ProdList
- 510
- Advantage
- 64
- Tel
- 0531-88811783
- Fax
- +86 (531) 55696010 QQ 1762738062
- sales@trio-pharmatech.com
- Country
- China
- ProdList
- 1856
- Advantage
- 62
- Tel
- 4009903999 13355009207
- Fax
- 0539-6365991
- 3007715519@qq.com
- Country
- China
- ProdList
- 18729
- Advantage
- 57
- Tel
- 0086-21-58956006
- Fax
- 0086-21-58956100
- Country
- China
- ProdList
- 7811
- Advantage
- 57
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4747
- Advantage
- 58
- Tel
- 025-66113011 17798518460
- Fax
- (1)02557626880
- cfzhang@aikonchem.com
- Country
- China
- ProdList
- 19913
- Advantage
- 55
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
View Lastest Price from RG108 manufacturers
- Product
- RG108 48208-26-0
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98
- Supply Ability
- 10000KGS
- Release date
- 2025-12-03
- Product
- RG108/RG-108 48208-26-0
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 20kg
- Release date
- 2019-09-05