How do you dissolve wortmannin?
A stock solution may be made by dissolving the wortmannin in an organic solvent purged with an inert gas. Wortmannin is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF).
What are PI3K inhibitors used for?
What are PI3K inhibitors used for? PI3K inhibitors are usually given to treat certain cancers that have relapsed or are unresponsive to other cancer treatments. Typically, at least two other cancer treatments need to have been tried and been unsuccessful or not tolerated before PI3K inhibitors are given.
What happens if Akt is inhibited?
Akt inhibitor LY2780301 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway, thereby leading to inhibition of cell proliferation and the induction of apoptosis in tumor cells.
Is PI3K phosphorylated?
Results: We found that PI3K regulatory subunit p85 was predominantly phosphorylated in radioresistant head and neck cancer cell line (HN31), which showed resistance to PI3K inhibitors. Next, we investigated mechanism through which PI3K p85 phosphorylation modulated response to PI3K inhibitors.
What kind of metabolite is wortmannin and what is its role?
Wortmannin is an organic heteropentacyclic compound, a delta-lactone, an acetate ester and a cyclic ketone. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an anticoronaviral agent. Wortmannin is a steroid metabolite of Penicillium funiculosum and Talaromyces wortmannii fungi.
What kind of enzyme does wortmannin inhibit?
Wortmannin is a steroid metabolite of _Penicillium funiculosum_ and _Talaromyces wortmannii_ fungi. This drug acts as a nonspecific, covalent inhibitor of phosphoinositide 3-kinase enzymes (PI3Ks).
What is the concentration of Wortmannin in dimethylsulfoxide?
Wortmannin and LY294002 (Calbiochem, San Diego, CA) were dissolved in dimethylsulfoxide at a concentration of 1 mM for worthmannin and 50 mM for LY294002 and stored at −70°C. Stock solutions were diluted immediately before use in medium to a final concentration of 1 mM and 50 mM, respectively.
How does wortmannin work as a selective inhibitor of PI3K?
Wortmannin is a fungal metabolite that was identified as a potent and selective inhibitor for phosphoinositide 3-kinases (PI3Ks) and PI3K-related enzymes.144,145 Kinases of this family covalently react via a conserved active site lysine nucleophile with an electrophilic extended Michael acceptor system in wortmannin.