RG 108

RG 108 (CAS 48208-26-0)

RG 108 | CAS 48208-26-0 is rated 5.0 out of 5 by 1.
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Synonym: DNA Methyltransferase Inhibitor
Application: A Dnmt inhibitor that silences tumor suppressor genes
CAS Number: 48208-26-0
Purity: ≥97%
Molecular Weight: 334.33
Molecular Formula: C19H14N2O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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RG 108 is a non-nucleoside DNA methyltransferase (Dnmt) inhibitor that blocks the enzyme active site. RG 108 inhibits DNA methylation in human cancer cell lines without detectable toxicity in vitro. The compound demethylates and reactivates epigenetically silences tumor suppressor genes.


References

Brueckner et al (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of DNA methyltransferase. Cancer Res. 65 6305. Stresemann et al (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res. 66 2794. Schirrmacher et al (2006) Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug.Chem. 17 261.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), water (<1 mg/ml at 25° C), ethanol (67 mg/ml at 25° C), and DMF (~30 mg/ml).
Storage :
Store at -20° C
Melting Point :
271.38° C (Predicted)
Boiling Point :
605.99° C at 760 mmHg (Predicted)
Density :
1.50 g/cm3 (Predicted)
Refractive Index :
n20D 1.74 (Predicted)
Optical Activity :
α20/D -319.8°, c = 1 in ethanol
IC50 :
DNA methyltransferase: IC50 = 115 nM
Ki Data :
CpG DNA methylase: Ki= 230 nM (Spiroplasma monobiae)
pK Values :
pKa: 3.62 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
16079004
MDL Number :
MFCD08705332
SMILES :
C1CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Mitchnick KA; et al Mitchnick KA; et al. (PubMed ID: 25639476) exhibited that RG-108, a DNA methyltransferase inhibitor, diminished long-term object-in-place memory in hippocampus and perirhinal cortex. -SCBT Publication Review
Date published: 2015-04-01
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