Wortmannin, >99%

Catalog Number: W-2990
Synonyms : [KY 12420]
M.W. 428.43
C23H24O8
[19545-26-7]
M.I. 12: 10188
M.I. 14: 10053

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO or ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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Isolated from the filamentous fungus, Penicillium funiculosum, wortmannin is a potent, irreversible, and specific inhibitor of phosphatidylinositol 3-kinase (PI3-K) with an IC50 of 2-5 nM. Arcaro, A., and Wymann, M.P. "Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses." Biochem. J. 296: 297-301 (1993). Wymann, M.P., and Arcaro, A. "Platelet-derived growth factor-induced phosphatidylinositol 3-kinase activation mediates actin rearrangements in fibroblasts." Biochem. J. 298: 517-520 (1994). Powis, G., et al. "Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase." Cancer Res. 54: 2419-2423 (1994). Wymann, M.P., et al. "Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction." Mol. Cell Biol. 16: 1722-1733 (1996).
Inhibitor of both myosin light chain kinase (IC50 = 200 nM) and phosphatidylinositol 4-kinase at concentrations approximately 100-fold higher than the that required for PI3-K inhibition. Nakanishi, S., et al. "Wortmannin, a microbial product inhibitor of myosin light chain kinase." J. Biol. Chem. 267: 2157-2163 (1992).
Enhances radiation- or serum withdrawal-induced apoptosis through the inhibition of PI3-K/Akt signal transduction cascade and blocks the antiapoptotic effect of cytokines. Krasilnikov, M., et al. "Contribution of phosphatidylinositol 3-kinase to radiation resistance in human melanoma cells." Mol. Carcinog. 24: 64-69 (1999). Allen, M.P., et al. "Growth arrest-specific gene 6/adhesion related kinase signaling promotes gonadotropin-releasing hormone neuronal survival via extracellular signal-regulated kinase (ERK) and Akt." Mol. Endocrinol. 13: 191-201 (1999). Morita, Y., et al. "Requirement for phosphatidylinositol-3'-kinase in cytokine-mediated germ cell survival during fetal oogenesis in the mouse." Endocrinology 140: 941-949 (1999). Manna, S.K., and Aggarwal, B.B. "Interleukin-4 down-regulates both forms of tumor necrosis factor receptor and receptor-mediated apoptosis, NFkappaB, AP-1, and c-Jun N-terminal kinase." J. Biol. Chem. 273: 33333-33341 (1998). Crowder, R.J., and Freeman, R.S. "Phosphatidylinositol 3-kinase and Akt protein kinase are necessary and sufficient for the survival of nerve growth factor-dependent sympathetic neurons." J. Neurosci. 18: 2933-2943 (1998).
Wortmannin inhibition of PI3-K also blocks many of the short-term metabolic effects induced by insulin receptor activation in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Okada, T., et al. "Essential role of phosphatidylinositol 3-kinase in insulin-induced glucose transport and antilipolysis in rat adipocytes. Studies with a selective inhibitor wortmannin." J. Biol. Chem. 269: 3568-3573 (1994). Moule, S.K., and Denton, R.M. "Multiple signaling pathways involved in the metabolic effects of insulin." Am. J. Cardiol. 80: 41A-49A (1997).
Inhibits platelet activating factor-induced MAP kinase activation in guinea pig neutrophils (200 - 300 nM). Ferby, I.M., et al. "Wortmannin inhibits mitogen-activated protein kinase activation induced by platelet-activating factor in guinea pig neutrophils." J. Biol. Chem. 269: 30485-30488 (1994).
Inhibits phospholipase D activation. Bonser, R.W., et al. "Demethoxyviridin and wortmannin block phospholipase C and D activation in the human neutrophil." Br. J. Pharmacol. 103: 1237-1241 (1991).
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

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