RG108 - 10mM in DMSO , CAS No.48208-26-0

CAS: 48208-26-0 Cat. No.: R408948 Peso molecular: 334.33 PubChem CID: 702558

GRADE & PURITY 10mM in DMSO

Synonyms

N-Phthalyl-L-tryptophan | 1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

RG108 RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.
In vitro

RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences. In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes. In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs.

In vivo

Cell Data

cell lines：

Concentrations：1-100 μM

Incubation Time：5 days

Powder Purity:≥99%

Specifications

Sinónimos

N-Phthalyl-L-tryptophan | 1H-Indole-3-propanoic acid, α-(1, 3-dihydro-1, 3-dioxo-2H-isoindol-2-yl)-, (αS)-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Nombres e identificadores

• Isómeros SMILES: C1=CC=C2C(=C1)C(=O)N(C2=O)[C@@H](CC3=CNC4=CC=CC=C43)C(=O)O
• WGK Alemania: 3
• PubChem CID: 702558
• Peso molecular: 334.33
• Reaxy-Rn: 4552782

Objetivos asociados (humanos)

DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (1 Activities)

Discover Target: DNMT3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (1 Activities)

Discover Target: DNMT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Rotación específica [α]: -271° (C=1,EtOH)
• Punto de fusión (°C): 181 °C