Activin Receptor-like Kinase Inhibitor

1

　SB431542 (1) is a specific and potent inhibitor of the activin receptor-like kinase (ALK) family, e.g., ALK4, ALK5, ALK7.¹⁾ 1 can also inhibit TGF-β-mediated activation of SMAD and induction of fibronectin and collagen expression in TGF-β-response cell lines.²⁾
　Since Yamanaka et al. identified reprogramming factors for iPS (induced pluripotent stem) cells from somatic sells,³⁾ chemical substitutes for these factors have also been developed.^4,5) 1 can also replace Sox2, in reprogramming mouse fibroblasts to iPS cells.⁶⁾

The product is for research purposes only.

　

References

• 1) SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7
  • G. J. Inman, F. J. Nicolás, J. F. Callahan, J. D. Harling, L. M. Gaster, A. D. Reith, N. J. Laping, C. S. Hill, Mol. Pharmacol. 2002, 62, 65.
• 2) Inhibition of transforming growth factor (TGF)-β1–induced extracellular matrix with a novel inhibitor of the TGF-β type I receptor kinase activity: SB-431542
  • N. J. Laping, E. Grygielko, A. Mathur, S. Butter, J. Bomberger, C. Tweed, W. Martin, J. Fornwald, R. Lehr, J. Harling, L. Gaster, J. F. Callahan, B. A. Olson, Mol. Pharmacol. 2002, 62, 58.
• 3) Induction of pluripotent stem cells from mouse embryonic and adult fibroblast cultures by defined factors
  • K. Takahashi, S. Yamanaka, Cell 2006, 126, 663.
• 4) Dissecting direct reprogramming through integrative genomic analysis
  • T. S. Mikkelsen, J. Hanna, X. Zhang, M. Ku, M. Wernig, P. Schorderet, B. E. Bernstein, R. Jaenisch, E. S. Lander, A. Meissner, Nature 2008, 454, 49.
• 5) Induction of pluripotent stem cells by defined factors is greatly improved by small-molecule compounds
  • D. Huangfu, R. Maehr, W. Guo, A. Eijkelenboom, M. Snitow, A. E. Chen, D. A. Melton, Nat. Biotech. 2008, 26, 795.
• 6) A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog
  • J. K. Ichida, J. Blanchard, K. Lam, E. Y. Son, J. E. Chung, D. Egli, K. M. Loh, A. C. Carter, F. P. Di Giorgio, K. Koszka, D. Huangfu, H. Akutsu, D. R. Liu, L. L. Rubin, K. Eggan, Cell Stem Cell 2009, 5, 491.

Page Top