ChemicalBook > CAS DataBase List > RG108

RG108

Product Name
RG108
CAS No.
48208-26-0
Chemical Name
RG108
Synonyms
108;CS-1518;RG108 >98%;RG108/RG-108;RG108 USP/EP/BP;N-Phthalyl-L-tryptophan;N-Phthaloyl-L-tryptophan;N-Phthalyl-L-tryptophan>DNA Methyltransferase Inhibitor;RG-108;RG 108;N-PHTHALYL-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

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J & K SCIENTIFIC LTD.
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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)-
  • 48208-26-0
  • Inhibitors
  • DNA Methyltransferase Inhibitor
  • Epigenetics