Stemgent Stemolecule ALK5 Inhibitor (RepSox)

Code: 04-0015-base
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Stemolecule ALK5 Inhibitor, also known as RepSox, E 616452, and SJN 2511, is a selective and ATP-competitive inhibitor of the TGFβ family type I receptor activin receptor-like kinase (ALK5)1. The ALK5 Inhibitor works by preventing autophosphorolation of ALK5. It has also been shown that ALK5 can replace Sox2 when reprogramming cells to induced pluripotent stem (iPS) cells. Through inhibition of the TGFβ pathway, ALK5 works to reprogram cells that have been transduced with Oct4, Klf4, and c-Myc2.

Product Name

Stemolecule ALK5 Inhibitor (RepSox)

Catalog Number

04-0015

Size

1 mg

Alternate Name(s)

  • RepSox
  • E 616452
  • SJN 2511
  • 2-(3-(6-methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine

Chemical Formula

C17H13N5

Molecular Weight

287.32

CAS Number

446859-33-2

Purity

Greater than 99% by HPLC analysis

Formulation

Yellow solid

Solubility

For a 10 mM concentrated stock solution of ALK5 Inhibitor, reconstitute the compound by adding 348 µL 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 methanol at 17 mM.

Storage and Stability

Store powder at 4 °C or lower, 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. The effect of storage of stock solutions should be verified for each application.

Quality Control

The purity of ALK5 Inhibitor was determined by HPLC analysis. The accurate mass was determined by mass spectrometry. Cellular toxicity of ALK5 Inhibitor was tested on HeLa and HEK293 cells.

Specification Sheets

Safety Data Sheets

  1. Li, W., Wei, W., Zhu, S., Zhu, J., Shi, Y., Lin, T., Hao, E., Hayek, A., Deng, H., and Ding, S. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4: 16-19 (2009).
  2. Gellibert, F., Woolven, J., Fouchet, M. H., Mathews, N., Goodland, H., Lovegrove, V., Laroze, A., Nguyen, V. L., Sautet, S., Wang, R., Janson, C., Smith, W., Krysa, G., Boullay, V., De Gouville, A. C., Huet, S., and Hartley, D. Identification of 1, 5-naphthyridine derivatives as a novel series of potent and selective TGFβ type I receptor inhibitors. J Med Chem 47: 4494-4506 (2004).
  3. Ichida, J.K., Blanchard, J., Lam, K., Son, E.Y., Chung, J.E., Egli, D., Loh, K.M., Carter, A.C., Di Giorgio, F.P., Koszka, K., Huangfu, D., Akutsu, H., Liu, D.R., Rubin, L.L., and Eggan, K. A small-molecule inhibitor of Tgf-? signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 5: 491-503 (2009).

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