Wortmannin

By phosphorylating phosphatidylinositol, phosphoinositide 3-kinases (PI3K), activates diverse cellular functions, including cell growth, differentiation, survival, and motility. Wortmannin is a potent, cell-permeable, and irreversible inhibitor of PI3K enzymes (IC₅₀ = 1-10 nM). However, the class II PI3Ks from Drosophila, murine, and human differ in sensitivity to wortmannin (IC₅₀s = 5, 50, 450 nM, respectively).¹ Wortmannin also inhibits polo-like kinase 1 (IC₅₀ = 24 nM) and polo-like kinase 3 (IC₅₀ = 49 nM), as well as mTOR, DNA-PK, PI4K, MLCK, and p38 MAPK at 50 to 100 fold higher concentrations than that needed for PI3K inhibition.^2,3

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1. Fruman, D.A., Meyers, R.E., and Cantley, L.C. Phosphoinositide kinases. Annu. Rev. Biochem. 67, 481-507 (2008).

2. Liu, Y., Shreder, K.R., Gai, W., et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem. Biol. 12, 99-107 (2005).

3. Liu, Y., Jiang, N., Wu, J., et al. Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects. The Journal of Biological Chemisty 282(4), 2505-2511 (2007).

Liu, A., Guo, E., Yang, J., et al. Young plasma reverses age-dependent alterations in hepatic function through the restoration of autophagy. Aging Cell 17(1), e12708 (2018).

McDougle, D.R., Watson, J.E., Abdeen, A.A., et al. Anti-inflammatory ω-3 endocannabinoid epoxides. Proc. Natl. Acad. Sci. USA 114(30), E6034-E6043 (2017).