Stemolecule RG108

Catalog 04-0001
Size 10 mg
Price
$135.00
$135.00
Availability In stock
Catalog
04-0001

Product Overview

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 andin 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 Specifications

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 soluble in DMSO at 100 mM and ethanol at 100 mM.
Storage and Stability
Store lypholized 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


References

  1. Brueckner, B., Boy, R., Siedlecki, P., Musch, T., Kliem, H., Zielenkiewicz, P., Suhai, S., Wiessler, M., and Lyko, F. (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res
  2. Stresemann, C., Brueckner, B., Musch, T., Stopper, H., and Lyko, F. (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res 66: 2794-2800.
  3. Shi, Y., Desponts, C., Do, J.T., Hahm, H.S., Schöler, H.R., and Ding, S. (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3: 568-574.

Additional Publications

Product Specifications

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 soluble in DMSO at 100 mM and ethanol at 100 mM.
Storage and Stability
Store lypholized 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

References

  1. Brueckner, B., Boy, R., Siedlecki, P., Musch, T., Kliem, H., Zielenkiewicz, P., Suhai, S., Wiessler, M., and Lyko, F. (2005) Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res
  2. Stresemann, C., Brueckner, B., Musch, T., Stopper, H., and Lyko, F. (2006) Functional diversity of DNA methyltransferase inhibitors in human cancer cell lines. Cancer Res 66: 2794-2800.
  3. Shi, Y., Desponts, C., Do, J.T., Hahm, H.S., Schöler, H.R., and Ding, S. (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3: 568-574.

Additional Publications