General description

A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 µM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC₅₀ = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC₅₀ ≥10 µM in the presence of 10 µM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ikushima, H., et al. 2009. Cell Stem Cell5, 504.Lin, T., et al. 2009. Nat. Methods6, 805.Maherali, N. and Hochedlinger, K., 2009. Curr. Biol.19, 1718.Callahan, J.F., et al. 2002. J. Med. Chem.45, 999.Inman, G.J., et al. 2002. Mol. Pharmacol.62, 65.Laping, N.J., et al. 2002. Mol. Pharmacol.62, 58.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 100 mM (5 mg/119 µl) solution of SB431542 (Cat. No. 616461) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Irritant (B)