Stemgent Stemolecule RG108

Code: 04-0001-base
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Stemolecule RG108 is a cell-permeable small molecule that inhibits DNA methyltransferases. Treatment with RG108 results in the demethylation of genomic DNA and can reactivate epigenetically silenced tumor suppressor genes, making it a great tool for studying methlytransferase biological functions in vivo and in vitro1,2. It is particularly useful due to its non-covalent binding to the enzyme activation domain, which makes the inhibition reversible. Along with BIX01294, RG108 has been shown to improve the reprogramming efficiency of mouse embryonic fibroblasts (MEFs) into induced pluripotent stem (iPS) cells3. RG108 can potentially be used to maintain embryonic stem (ES) cells in an undifferentiated state as well as replace transcription factors in both mouse and human cell reprogramming.

Product Name

Stemolecule RG108

Catalog Number

04-0001

Size

10 mg

Alternate Name(s)

2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propionic acid

Chemical Formula

C19H14N2O4

Molecular Weight

334.44

CAS Number

48208-26-0

Purity

Greater than 99% by HPLC analysis

Formulation

Yellow solid

Solubility

For a 10 mM concentrated stock solution of RG108, reconstitute the compound by adding 2.99 mL of DMSO to the entire contents of the vial. If precipitate is observed, warm the solution to 37 °C for 2 to 5 minutes. For cell culture, the media should be prewarmed prior to adding the reconstituted compound. Note: for most cells, the maximum tolerance to DMSO is less than 0.5%. This molecule is reported to be soluble in DMSO at 100 mM and ethanol at 100 mM.

Storage and Stability

Store lyopholized powder at 4 °C protected from light. Information about the stability of Stemolecules in solution is largely not available. As a general guideline, we recommend that stock solution be freshly made and stored in aliquots at −20 °C, protected from light. The effect of storage of stock solutions should be verified for each application.

Quality Control

The purity of RG108 was determined by HPLC analysis. The accurate mass was determined by mass spectrometry. Cellular toxicity of RG108 was tested on mouse embryonic stem cells.

Specification Sheets

Safety Data Sheets

  1. Brueckner, B., Boy, R., Siedlecki, P., Musch, T., Kliem, H., Zielenkiewicz, P., Suhai, S., Wiessler, M., and Lyko, F. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res65:6305-11 (2005).
  2. Stresemann, C., Brueckner, B., Musch, T., Stopper, H., and Lyko, F. Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res66: 2794-2800 (2006).
  3. Shi, Y., Desponts, C., Do, J.T., Hahm, H.S., Schöler, H.R., and Ding, S. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3: 568-574 (2008).

Additional Publications

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