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;N-Phthalyl-L-tryptophan;N-Phthaloyl-L-tryptophan;N-Phthalyl-L-tryptophan>N-phthalimide-L-tryptophan
CBNumber: CB0972112
Molecular Formula: C19H14N2O4
Formula Weight: 334.33
MOL File: 48208-26-0.mol

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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
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

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Safety

WGK Germany: 3
HS Code: 2933.99.9701

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: R8279
Product name: RG108
Purity: ≥98% (HPLC), powder
Packaging: 10mg
Price: $271
Updated: 2024/03/01

TCI Chemical

Product number: P2023
Product name: N-Phthalyl-L-tryptophan
Purity: >98.0%(HPLC)(T)
Packaging: 50mg
Price: $153
Updated: 2024/03/01

TCI Chemical

Product number: P2023
Product name: N-Phthalyl-L-tryptophan
Purity: >98.0%(HPLC)(T)
Packaging: 200mg
Price: $454
Updated: 2024/03/01

Alfa Aesar

Product number: J64630
Product name: DNA Methyltransferase Inhibitor
Packaging: 10mg
Price: $176
Updated: 2023/06/20

Cayman Chemical

Product number: 13302
Product name: RG-108
Purity: ≥98%
Packaging: 5mg
Price: $62
Updated: 2024/03/01

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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.

storage

Room temperature

References

1) Brueckner et al. (2005), Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferase; Cancer Res., 65 6305 2) Stresemann et al. (2006), Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines; Cancer Res., 66 2794 3) Szablowska-Gadomska et al. (2012), Treatment with small molecules is an important milestone towards the induction of pluripotency in neural stem cells derived from human cord blood; Acta Neurobiol. Exp., 72 337

RG108 Preparation Products And Raw materials

Raw materials

Preparation Products

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RG108 Suppliers

Canada 1 China 114 India 3 Japan 1 Switzerland 1 United Kingdom 4 United States 23 Global 147

VDM Biochemicals

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View Lastest Price from RG108 manufacturers

Career Henan Chemical Co

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

48208-26-0, RG108Related Search:

TRICHOSTATIN A GSK J1 Vorinostat diethyl 1-benzyl-1,4-dihydro-4-phenylpyridine-3,5-dicarboxylate 5-Aza-2'-deoxycytidine SB 431542 GSK 343 5-Azacytidine SGI-1027 BEZ235 (NVP-BEZ235, Dactolisib) [2-(1 H-INDOL-3-YL)-ETHYL]-(2-METHYL-BENZYL)-AMINE BZ-TRP-OH RG108

(S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid

RG108/RG-108

(S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid

N-Phthaloyl-L-tryptophan

1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-

N-Phthaloyl-L-tryptophan (S)-3-(Indol-3-yl)-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)propanoic acid

CS-1518

DNA Methyltransferase Inhibitor

N-Phthalyl-L-tryptophan

RG108 >98%

RG108/DNA Methyltransferase Inhibitor/N-Phthalyl-L-tryptophan

2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid

RG-108;RG 108;N-PHTHALYL-L-TRYPTOPHAN

N-Phthalyl-L-tryptophan&gt

108

RG108 USP/EP/BP

1H-Indole-3-propanoicacid, a-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-,(aS)-

N-phthalimide-L-tryptophan

R 108

48208-26-0

Inhibitors

DNA Methyltransferase Inhibitor

Epigenetics