Biochem/physiol Actions

Secondary TargetCOX-2 (IC₅₀ = 27 nM)

Primary Targetp60^v-src kinase activity

General description

A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60^v-src kinase activity (IC₅₀ = 0.27 nM). Inhibits the expression of COX-2 (IC₅₀ = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts K-Ras-activated signaling pathways by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56^lyn in LPS-stimulated macrophages. Suppresses NIH/3T3 cell transformation by diverse oncogenes such as src, ras, and mos in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Inhibits Wnt-5A expression in dermal papilla cells (IC₅₀ = 190 nM).

A cell-permeable, ATP-site binding, and irreversible antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60^v-src kinase activity (IC₅₀ = 0.27 µM). Inhibits the expression of COX-2 (IC₅₀ = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts k-Ras-activated signaling pathway by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56^lyn in LPS-stimulated macrophages. Suppresses NIH 3T3 cell transformation by diverse oncogenes, such as src, ras and mos, at least in part by blocking the key signal transduction intermediates, such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Inhibits Wnt-5A expression in dermal papilla cells (IC₅₀ = 190 nM).

Legal Information

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

Other Notes

Shinonaga, H., et al. 2009. Bioorg. Med. Chem.17, In press.Soga, S., et al. 1998. J. Biol. Chem. 273, 822.Chanmugam, P., et al. 1995. J. Biol. Chem. 270, 5418.Shimada, Y., et al. 1995. J. Antibiot. 48, 824.Zhao, J.F., et al. 1995. Oncogene 11, 161.Oikawa, T., et al. 1993. Eur. J. Pharmacol. 241, 221.Kwon, H.J., et al. 1992. Cancer Res. 52, 6926.

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Warning

Toxicity: Harmful (C)