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Soluble in DMSO. SB-431542 selectively inhibited Smad3 phosphorylation, with an IC50 of 94 nM. It also blocked TGF-beta1-induced nuclear Smad3 localization. Laping N.J., et al. 'Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542.' Mol. Pharmacol. 62: 58-64 (2002). SB-431542 is a potent inhibitor of activin receptor-like kinase (ALK)5 (the TGF-beta type I receptor). It also inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7. It has no major effect on the other ALK family members that recognize bone morphogenetic proteins (BMPs). Inman G.J., et al. '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.' Mol. Pharmacol. 62: 65-74 (2002). SB-431542 is a specific inhibitor of TGF-beta receptor kinase. It inhibits TGF-beta-induced transcription, gene expression and tumor-promoting effects. Interestingly, SB-431542 promoted anchorage independent growth of cells which were growth-inhibited by TGF-beta, whereas it inhibited colony formation by cells which were growth-promoted by TGF-beta. Halder S.K., et al. 'A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers.' Neoplasia. 7: 509-521 (2005).
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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