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RG108

RG108 structure

CAS No:
48208-26-0
Formula:
C19H14N2O4
Chemical Name:
RG108
Synonyms:
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;(S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid;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;DNA Methyltransferase Inhibitor;N-Phthalyl-L-tryptophan
Categories:
Biochemical Engineering > Inhibitors

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Description

RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.

(2S)-2-(1,3-dioxo-2-isoindolyl)-3-(1H-indol-3-yl)propanoic acid is an indolyl carboxylic acid.

RG108 Basic Attributes

Molecular Weight：

334.33

Exact Mass：

334.095367

Characteristics

PSA：

90.5

XLogP3：

2.6

Appearance：

yellow

Density：

1.5±0.1 g/cm3

Melting Point：

192-194℃

Boiling Point：

670.3°C at 760 mmHg

Flash Point：

320.3±30.1 °C

Refractive Index：

1.741

Water Solubility：

DMSO: >10mg/mL

Storage Conditions：

Store at RT

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

Drug Information

MeSH Entry Terms：

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

RG108 Use and Manufacturing

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.

Computed Properties

Molecular Weight:334.3
XLogP3:2.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:4
Exact Mass:334.09535693
Monoisotopic Mass:334.09535693
Topological Polar Surface Area:90.5
Heavy Atom Count:25
Complexity:554
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Shaanxi Dideu Medichem Co. Ltd Contact Supplier

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48208-26-0 (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid

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Grade: Industrial Grade

Content: 95%

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Shanghai Beixinke Chemical Co., Ltd. Contact Supplier

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Trader Supplier of Pharmaceutical intermediates,high molecular polymers

RG 108,N-Phthalyl-L-tryptophan BXK

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