Wortmannin, a fungal metabolite, is a potent and selective inhibitor of phosphatidylinositol 3-kinase. This compound is active with purified preparations and cytosolic fractions and because it is highly cell-permeable, it is also suitable for use with intact cells. Several biological effects are observed with wortmannin treatment, including the inhibition of fMLP induced PIP3 and superoxide anion production in guinea pig neutrophils and the blockage of the metabolic effects of insulin in isolated rat adipocytes without effect on the insulin receptor tyrosine kinase activity. The mechanism of wortmannin’s inhibition of PI 3-kinase has been determined to be the formation of a covalent bond with its target. Wortmannin’s inhibition of PI 3-kinase is selective and inhibition of other kinases such as PI 4-kinase and myosin light chain kinase, occurs at concentrations 100 fold higher than those required for inhibition of PI 3-kinase.
Solubility:Soluble in DMSO or ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.
Melting Point:As reported
Elemental Analysis:As reported
Biological Activity:IC50= 5nM with purified preparations and cell fractions. IC50= 50nM by measuring PIP3 and superoxide production by guinea pig neutrophils.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with DMSO or ethanol. Make solutions fresh, immediately before use. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.
