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48208-26-0

  • Product Name:RG108
  • Molecular Formula:C19H14 N2 O4
  • Molecular Weight:334.331
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Product Details

pd_meltingpoint:192-194℃

Purity:99%

Cost-effective and customizable RG108 48208-26-0 factory

  • Molecular Formula:C19H14N2O4
  • Molecular Weight:334.331
  • Vapor Pressure:7E-19mmHg at 25°C 
  • Melting Point:192-194℃ 
  • Refractive Index:1.723 
  • Boiling Point:670.3°C at 760 mmHg 
  • PKA:3.62±0.10(Predicted) 
  • Flash Point:359.2°C 
  • PSA:90.47000 
  • Density:1.47g/cm3 
  • LogP:2.39770 

RG108(Cas 48208-26-0) Usage

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.

General Description

RG108, a non-nucleoside analog is also called [2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl) propanoic acid.

InChI:InChI=1/C19H16N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h3-8,10,16,20H,1-2,9H2,(H,24,25)/t16-/m0/s1

48208-26-0 Relevant articles

Convergent Synthesis of Calcium-Dependent Antibiotic CDA3a and Analogues with Improved Antibacterial Activity via Late-Stage Serine Ligation

Blasco, Pilar,Chen, Delin,Chen, Sheng,Li, Xuechen,Po, Kathy Hiu Laam

supporting information, (2020/06/29)

A convergent synthesis via the late-stag...

Chiral sensors for determining the absolute configurations of α-amino acid derivatives

Chen, Zhongxiang,Fan, Hongjun,Yang, Shiwei,Bian, Guangling,Song, Ling

, p. 6933 - 6939 (2018/10/02)

A simple strategy for configurational as...

Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan (RG108) as inhibitors of DNA methyltransferase 1

Asgatay, Saa?dia,Champion, Christine,Marloie, Ga?l,Drujon, Thierry,Senamaud-Beaufort, Catherine,Ceccaldi, Alexandre,Erdmann, Alexandre,Rajavelu, Arumugam,Schambel, Philippe,Jeltsch, Albert,Lequin, Olivier,Karoyan, Philippe,Arimondo, Paola B.,Guianvarc'H, Dominique

, p. 421 - 434 (2014/02/14)

DNA methyltransferases (DNMT) are promis...

Phthaloyl amino acids as anti-inflammatory and immunomodulatory prototypes

Leite, Ana Cristina Lima,Barbosa, Fabio Fernandes,Cardoso, Marcos Verissimo De Oliveira,Moreira, Diogo R. M.,Coelho, Lucas Cunha D.,Da Silva, Elany Barbosa,Filho, Gevanio Bezerra De Oliveira,De Souza, Valdenia Maria Oliveira,Pereira, Valeria Rego A.,Reis, Luiza De C.,Ferreira, Paulo Michel Pinheiro,Pessoa, Claudia,Wanderley, Almir Goncalves,Mota, Fernanda Virginia B.,Da Silva, Teresinha G.

, p. 1701 - 1708 (2014/05/06)

A series of phthalimide analogs were syn...

48208-26-0 Process route

N-ethoxycarbonylphthalimide
22509-74-6

N-ethoxycarbonylphthalimide

L-Tryptophan
73-22-3,27732-43-0,80206-30-0,27813-82-7

L-Tryptophan

N-phthalimide-L-tryptophan
32675-71-1,48208-26-0,62361-30-2

N-phthalimide-L-tryptophan

Conditions
Conditions Yield
L-Tryptophan; With sodium carbonate; In water;
N-ethoxycarbonylphthalimide; In water; at 20 ℃; for 2h;
98%
With sodium carbonate; In water; at 20 ℃; for 1h;
95%
With sodium carbonate; In water; at 20 ℃; for 5h;
L-Tryptophan
73-22-3,27732-43-0,80206-30-0,27813-82-7

L-Tryptophan

methyl 2-(N-succinimidyloxycarbonyl)benzoate
438470-19-0

methyl 2-(N-succinimidyloxycarbonyl)benzoate

N-phthalimide-L-tryptophan
32675-71-1,48208-26-0,62361-30-2

N-phthalimide-L-tryptophan

Conditions
Conditions Yield
L-Tryptophan; methyl 2-(N-succinimidyloxycarbonyl)benzoate; With sodium carbonate; In water; acetonitrile;
With hydrogenchloride; In water; acetonitrile;
100%
With sodium carbonate; In water; acetonitrile;
100%
With sodium carbonate; In water; acetonitrile; at 20 ℃;
26%
L-Tryptophan; methyl 2-(N-succinimidyloxycarbonyl)benzoate; With potassium carbonate; In N,N-dimethyl-formamide; at 100 ℃; for 3h;
With hydrogenchloride; In water; N,N-dimethyl-formamide; Product distribution / selectivity;

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