A non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity

RG-108 – 5 mg

Brand:
Cayman
CAS:
48208-26-0
Storage:
-20
UN-No:
Non-Hazardous - /

DNA methylation regulates gene expression in normal and malignant cells. RG-108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro).{17258} 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.{17257,17258} Further, RG-108 inhibits DNA methyltransferase activity by blocking the enzyme active site.{17257} Through these actions, RG-108 demethylates and reactivates epigenetically silenced tumor suppressor genes.{17258}  

 

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Description

A non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity

Formal name: α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-(αS)-1H-indole-3-propanoic acid

Synonyms:  N-Phthalyl-L-Tryptophan

Molecular weight: 334.3

CAS: 48208-26-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|DNA/RNA Methylation

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