A83-01 is a selective inhibitor of the TGF-β type I receptor ALK5, the Activin/Nodal receptor ALK4, and the nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). This molecule is more potent than SB431542 in its inhibition of ALK4, 5, and 7, and only weakly inhibits ALK1, 2, 3, and 6. A 83-01 inhibits the TGF-β-induced epithelial-to-mesenchymal transition (EMT) via the inhibition of Smad2 phosphorylation1. This small molecule has been used to generate rat and human iPS cells towards a mouse ES cell like self-renewal state2View Poster
Soluble in DMSO (100 mM). For a 10 mM concentrated stock solution, reconstitute the compound by adding 475 µl of DMSO to the entire contents of the vial. Note: for most cells, the maximum tolerance to DMSO is <0.5%.
Storage
Store at 4°C. Protect from light. Following reconstitution, store aliquots at -20°C.
Stability
Stock solutions stable at -20°C for 6 months
Quality Control
The purity of A83-01 was determined by HPLC analysis. The accurate mass and structure of A83-01 was determined by mass spectrometry and NMR, respectively. Cellular toxicity of A83-01 was tested on HeLa and HEK293 cells.
References
Tojo, M., Hamashima, Y., Hanyu, A., Kajimoto, T., Saitoh, M., Miyazono, K., Node, M., and Imamura, T. (2005). The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci 96, 791-800.