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RG 108
- Optical Purity: >98% e.e.
- Soluble in DMSO
- MF: C19H14N2O4
- MW: 334.33
Description
RG 108 is a DNA methyltransferase (DNMT) inhibitor that reduces DNA methylation in human cancer cell lines without detectable cytotoxicity in reported studies.
DNMT inhibition can reactivate epigenetically silenced genes and alter transcriptional programs. RG 108 is useful for studying DNA methylation, tumor suppressor gene reactivation and small-molecule enhancement of induced pluripotent stem cell generation.
Key Features
- Inhibits DNA methyltransferase activity
- Demethylates and reactivates epigenetically silenced genes
- Non-nucleoside epigenetic tool compound
- Used with BIX 01294 in iPS cell generation studies
Applications
- DNA methylation and epigenetics research
- Tumor suppressor gene reactivation assays
- Stem cell reprogramming studies
- Cancer cell transcriptional regulation models
Promotion: RG 108 is also part of an inhibitor set:
| Stem Cell RG-BIX inhibitor Set (Axon 5008) |
More Information
| Parent CAS No. | 48208-26-0 |
|---|---|
| Chemical Name | (S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoic acid |
| SMILES | C1=CC2C(C[C@H](N3C(=O)C4=CC=CC=C4C3=O)C(=O)O)=CNC=2C=C1 |&1:5,r| |
| MFCD | N.A. |
| InChi | 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)/t16-/m0/s1 |
| InChiKey | HPTXLHAHLXOAKV-INIZCTEOSA-N |
| CID | 702558 |
| Short Description | DNA MTase inhibitor |
References
- B Brueckner et al. Epigenetic Reactivation of Tumor Suppressor Genes by a Novel Small-Molecule Inhibitor of Human DNA Methyltransferases. Cancer Res. 2005, 65, 6305-6311.
- C Stresemann et al. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res 2006, 66(5), 2794-2800.
- Y Shi et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 2008, 3, 568-574.
- Y Shi et al. A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell Stem Cell. 2008, 2(6), 525-528.
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