SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.

By G. Inman, F. J. Nicolás, J. Callahan, J. Harling, L. Gaster, A. Reith, N. Laping, C. Hill. Molecular Pharmacology, 2002

1,765 citations recorded by the source corpus.

Subfields: Molecular Biology, Rheumatology

View Paper: https://www.semanticscholar.org/paper/28d35c1092c151a939212866b5d00586278d01a3

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In Molecular Biology

1. J. Massagué
2. A. Moustakas
3. C. Heldin
4. R. Derynck
5. G. Keller
6. L. Vallier
7. O. De Wever
8. M. Mareel

Citations in the corpus

• Cytostatic and apoptotic actions of TGF-β in homeostasis and cancer (2003, background): “In this regard, small molecule inhibitors such as SB-431542 have been developed that effectively impair the kinase activity of TβR”
• Stage-specific optimization of activin/nodal and BMP signaling promotes cardiac differentiation of mouse and human pluripotent stem cell lines. (2011, background): “4 mM) (Inman et al., 2002), a specific inhibitor of the Activin/Nodal/TGF-b pathway, to the BMP4 induced (no activin) cultures at daily intervals, beginning at the onset of EB formation.”
• TGF‐β activates Erk MAP kinase signalling through direct phosphorylation of ShcA (2007, methodology): “We also treated 3T3-Swiss cells with SB431542, a specific inhibitor of TbRI (Inman et al, 2002).”
• Role of tissue stroma in cancer cell invasion (2003, background): “A small organic molecule inhibitor (SB431 542) has been designed that specifically inhibits TGF-βRI kinase activity [228,229].”
• Activin/Nodal and FGF pathways cooperate to maintain pluripotency of human embryonic stem cells (2005, methodology): “The effect of different members of the TGF family on EB growth was assayed by adding 10 ng/ml Activin (R&D Systems or Peprotech), 50 ng/ml of mouse recombinant Nodal (R&D Systems), 1 ng/ml of TGF 1 (Peprotech) or 10 M SB431542 (Tocris).”
• TGFβ/activin/nodal signaling is necessary for the maintenance of pluripotency in human embryonic stem cells (2005, background): “…the TGFβ/activin/nodal branch of TGFβ signaling, ALK4/ALK5/ALK7 has also been implicated in activation of MAP kinases, including p38, Jnk and Erk, although the only one of these kinases to be significantly affected by SB431542 in previously reported in vitro assays was p38 (Inman et al., 2002).”
• TGF-beta and the Smad signaling pathway support transcriptomic reprogramming during epithelial-mesenchymal cell transition. (2005, methodology): “Laping, GlaxoSmithKline Pharmaceuticals, and has been shown to inhibit selectively the ALK-4/-5/7 protein kinase activity (Inman et al., 2002).”
• A Small Molecule Inhibitor of Tgf-β Signaling Replaces Sox2 in Reprogramming by Inducing Nanog (2009, background): “The small molecule SB431542 (Figure 3A) is known to inhibit Tgfbr1 kinase and is structurally distinct from RepSox (Inman et al., 2002).”