S-7800 SB431542, Free Base, >99%

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  • M.W. 384.39
  • C22H16N4O3
  • [301836-41-9]

Solubility: DMSO.

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  • 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).
  • Related CAS numbers: 1049727-65-2 for the monohydrate.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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