General description

A cell-permeable quinoxaline compound that acts as a potent, highly selective, ATP-competitive inhibitor against type I TGF-β receptor TβR-I/ALK5 (IC₅₀ = 14.3 nM), while exhibiting 4-fold less potency toward ALK4 (IC₅₀ = 58.5 nM) and little or no activity against ALK2/3/6 and a panel of 26 other commonly studied kinases (≤29% inhibition at 10 µM). Effectively blocks (by >95%) TGF-β1-induced Smad2/3 activation (2 µM in ELT-3 cultures) and nuclear localization (1 µM in RPTE cultures), as well as TGF-β1-dependent p3TP- and ARE-luciferase transcription (0.1 µM in HaCat cultures). SB-525334 is orally available and is shown to attenuate Bleomycin- and Puromycin-induced tissue fibrosis in mice and rats in vivo.

Legal Information

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

Other Notes

Higashiyama, H., et al. 2007. Exp. Mol. Pathol.83, 39.Grygielko, E.T., et al. 2005. J. Pharmacol. Exp. Ther.313, 943.

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Packaging

Packaged under inert gas

2 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°:C). Stock solution is stable for up to 3 months at -20°C.

Warning

Toxicity: Harmful (C)