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Wortmannin, a metabolite of the fungus Penicillium funiculosum, is a specific inhibitor of phosphoinositide 3-kinases (PI3Ks). It has an in vitro inhibitory concentration (IC50) of around 5 nM, making it a more potent inhibitor than LY294002, another commonly used PI3K inhibitor. It displays a similar potency in vitro for the class I, II, and III PI3K members although it can also inhibit other PI3K-related enzymes such as mTOR, DNA-PK, some phosphatidylinositol 4-kinases, myosin light chain kinase (MLCK) and mitogen-activated protein kinase (MAPK) at high concentrations [1],[2] Wortmannin has also been reported to inhbit members of the polo-like kinase family [3]. Wortmannin is a commonly used cell biology reagent that has been used previously in research to inhibit DNA repair, Receptor-mediated endocytosis and cell proliferation[citation needed].
[edit] References
- ^ Vanhaesebroeck B et al., (2001)SYNTHESIS AND FUNCTION OF 3-PHOSPHORYLATED INOSITOL LIPIDS. Annu Rev Biochem.
- ^ Ferby I et al., 1996. Adv Exp Med Biol. PAF-induced MAPK activation is inhibited by wortmannin in neutrophils and macrophages.
- ^ Liu Y et al., 2007. J. Biol Chem 282(4): 2505-11 Polo-like Kinases Inhibited by Wortmannin: LABELING SITE AND DOWNSTREAM EFFECTS
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