A Thioamide for the Potent Inhibition of TGF-β Signaling

A 83-01 is a thioamide which acts as a potent inhibitor of the TGF-β type I receptor superfamily activin-like kinases Activin-Like Kinase 4 (ALK4), 5 (ALK5), and 7 (ALK7), making it specific for the TGF-β/Activin A/Nodal branch of the TGF-β signaling pathway.^1,2) Inhibition with A 83-01 prevents phosphorylation of Smad2/3, which in turn leads to attenuation of TGF-β-mediated growth inhibition and epithelial-to-mesenchymal transition. A 83-01 is a common component of organoid culture media; where it is used in concert with other niche factors to promote self-differentiation and self-assembly of stem cells into functionalized structures resembling native structures in vivo.³⁾

Related Products

A3324

A 83-01

Related Product Category Pages

• Organoid Culture
• Serine/Threonine Kinase Inhibitors (Others)

References

• 1) The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β
  • M. Tojo, Y. Hamashima, A. Hanyu, T. Kajimoto, M. Saitoh, K. Miyazono, M. Node, T. Imamura, Cancer Sci. 2005, 96, 791.
• 2) TGF-β is an inducer of ZEB1-dependent mesenchymal transdifferentiation in glioblastoma that is associated with tumor invasion
  • J. V. Joseph, S. Conroy, T. Tomar, E. Eggens-Meijer, K. Bhat, S. Copray, A. M. E. Walenkamp, E. Boddeke, V. Balasubramanyian, M. Wagemakers, W. F. A. den Dunnen, F. A. E. Kruyt, Cell Death Dis. 2014, 5, e1443.
• 3) Long-term expansion of epithelial organoids from human colon, adenoma, adenocarcinoma, and Barrett's epithelium
  • T. Sato, D. E. Stange, M. Ferrante, R. G. J. Vries, J. H. van Es, S. van den Brink, W. J. van Houdt, A. Pronk, J. van Gorp. P. D. Siersema, H. Clevers, Gastroenterology 2011, 141, 1762.

Page Top