DNA methyltransferase inhibitor
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RG108

Item No. 13302

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αS-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1H-indole-3-propanoic acid
CAS Number
48208-26-0
Synonyms
  • N-Phthalyl-L-Tryptophan
Molecular Formula
C19H14N2O4
Formula Weight
334.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 50 mg/mlEthanol:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
220, 283 nm
SMILES
O=C1N([C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C(C4=C1C=CC=C4)=O
InChi Code
InChI=1S/C19H14N2O4/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/h1-8,10,16,20H,9H2,(H,24,25)
InChi Key
HPTXLHAHLXOAKV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

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    50 mg

    $525

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    100 mg

    $918

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    Cayman Chemical
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    Product Description

    DNA methylation regulates gene expression in normal and malignant cells. RG108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro).1 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.2,1 Further, RG108 inhibits DNA methyltransferase activity by blocking the enzyme active site.2 Through these actions, RG108 demethylates and reactivates epigenetically silenced tumor suppressor genes.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brueckner, B., Boy, R.G., Siedlecki, P., et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 65(14), 6305-6311 (2005).

    2. Stresemann, C., Brueckner, B., Musch, T., et al. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66(5), 2794-2800 (2006).