General description
A naturally isolated cell-permeable fungal resorcylic lactone that acts as a selective and highly potent inhibitor against the MAPKKK TAK1 activity (IC50 = 8 nM) in an ATP-competitive and irreversible manner, while inhibiting MEK1 (IC50 = 411 nM) and three other MAPKKKs (IC50 ≥268 nM against MEKK1, ASK1, and MEKK4) only at much higher concentrations. Shown to inhibit IL-1-induced/TAK1-mediated, but not H2O2-induced/TAK1-independent, JNK and p38 phosphorylation in 293 cells. (5Z)-Zeaenol, Curvularia sp.(Cat. No. 499609) may serve as a negative control.
A naturally isolated cell-permeable fungal resorcylic lactone that acts as a selective and highly potent inhibitor against the MAPKKK TAK1 activity (IC50 = 8 nM) in an ATP-competitive and irreversible manner, while inhibiting MEK1 (IC50 = 411 nM) and three other MAPKKKs (IC50 ≥268 nM against MEKK1, ASK1, and MEKK4) only at much higher concentrations. Shown to inhibit IL-1-induced/TAK1-mediated, but not H2O2-induced/TAK1-independent, JNK and p38 phosphorylation in 293 cells. (5Z)-Zeaenol, Curvularia sp. (Cat. No. 499609) may serve as a negative control.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Windheim, M., et al. 2007. Biochem. J.404, 179.Choo, M.K., et al. 2006. Mol. Cancer Ther.5, 2970.Safwat, N., et al. 2005. Endocrinology146, 4814.Ninomiya-Tsuji, J., et al. 2003. J. Biol. Chem.278, 18485.Rawlins, P., et al. 1999. Int. J. Immunopharmacol.21, 799.
Packaging
1 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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