Description
Details
RG108 is an epigenetic modifier that inhibits DNA methyltransferase by blocking the enzyme active site (IC50 = 115 nM). It has been shown to enhance reprogramming efficiency of human and mouse somatic cells to induced pluripotent stem cells. RG108 has also been used for demethylation and reactivation of epigenetically silenced tumor suppressor genes.
Details
Details
| Molecular Weight | 334.33 |
|---|---|
| Molecular Formula | C19H14N2O4 |
| Chemical Name | (2S)-2-(1,3-dioxoisoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid |
| CAS Number | 48208-26-0 |
| PubChem Identifier | 702558 |
| Appearance | Brown solid |
| Purity | >99% by HPLC analysis |
| Solubility | Soluble in DMSO at 100 mM and ethanol at 100 mM |
| Reconstitution | For a 10 mM concentrated stock solution, reconstitute the compound by adding 1495.5 μL of DMSO to the entire contents of vial. If precipitate is observed, warm the solution to 37°C for 2 to 5 minutes. |
| Storage and Stability | Solid: Shipped at room temperature. Store at -20°C. Stable for 6 months when stored as directed. Solution: Following reconstitution, store aliquots in tightly sealed vials at -20°C. Avoid repeated freeze-thaw cycles. |
| References | Brueckner, B., et al. (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res 65(14): 6305-6311. PMID: 16024632. Mali, P., et al. (2010) Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes. Stem Cells 28(4): 713-720. PMID: 20201064. Shi, Y., et al. (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3(5): 568-574. PMID: 18983970. Stresemann, C., et al. (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res 66(5): 2794-2800. PMID: 16510601. |
| Technical Documents |