Wortmannin

Biochem/physiol Actions

Reversible: no

Target IC₅₀: 5 nM against phosphatidylinositol 3-kinase; 5 nM against PDGF-mediated Ins(3,4,5)P3 formation; 200 nM against myosin light chain kinase

Product does not compete with ATP.

Primary Targetphosphatidylinositol-3-kinase

Cell permeable: yes

General description

A fungal metabolite that acts as a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) in purified preparations and cytosolic fractions (IC₅₀ = 5 nM). Preincubation of fibroblasts with wortmannin abolishes PDGF-mediated Ins(3,4,5)P₃ formation (IC₅₀ = 5 nM). Blocks the catalytic activity of PI 3-kinase without affecting the upstream signaling events. Also blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Inhibits MAP kinase activation induced by platelet activating factor in guinea pig neutrophils (0.2-0.3 µM). Inhibits osteoclastic bone resorption. Inhibits other kinases, such as myosin light chain kinase (IC₅₀ = 200 nM) and PI 4-kinase at concentrations 100-fold higher than that required for the inhibition of PI 3-kinase. Also blocks phospholipase D.

A cell-permeable, fungal metabolite that acts as a potent, selective, and irreversible inhibitor of phosphatidylinositol 3-kinase in purified preparations and cytosolic fractions (IC₅₀ = 5 nM). Blocks the catalytic activity of PI 3-kinase without affecting the upstream signaling events. Preincubation of fibroblasts with wortmannin abolishes PDGF-mediated Ins(3,4,5)P₃ formation (IC₅₀ = 5 nM). Also blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Inhibits MAP kinase activation induced by platelet activating factor in guinea pig neutrophils (200 - 300 nM). Also inhibits other kinases such as myosin light chain kinase (IC₅₀ = 200 nM) and PI 4-kinase at concentrations higher than that required for inhibition of PI 3-kinase. Also blocks phospholipase D. A 10 mM (1 mg/233 µl) solution of Wortmannin (Cat. No. 681676) in DMSO is also available.

Legal Information

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

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Cross, M.J., et al. 1995. J. Biol. Chem. 270, 25352.Nakamura, I., et al. 1995. FEBS Lett. 361, 79.Ferby, I.M., et al. 1994. J. Biol. Chem. 269, 30485.Okada, T., et al. 1994. J. Biol. Chem. 269, 3568.Wymann, M.P. and Arcaro, A. 1994. Biochem. J.298, 517.Arcaro, A. and Wymann, M.P. 1993. Biochem. J.296, 297.Nakanishi, S., et al. 1992. J. Biol. Chem. 267, 2157.Bonser, R.W., et al. 1991. Br. J. Pharmacol.103, 1237.

Packaging

Packaged under inert gas

1 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Warning

Toxicity: Highly Toxic (H)