wortmannin

Description: Wortmannin (SL2052; KY12420), a steroid metabolite of the fungi Penicillium funiculosum, is the first described, potent selective and irreversible PI3K inhibitor with potential anticancer activity. It has an IC50 of 3 nM for inhibiting PI3K in a cell-free assay, but has little selectivity within the PI3K family proteins. It also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin is a steroid metabolite of the fungi Penicillium funiculosum, Talaromyces (Penicillium) wortmannii, is a specific, covalent inhibitor of phosphoinositide 3-kinases (PI3Ks) and Polo-Like kinase 1 (PLK1). 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. Wortmannin has also been reported to inhibit members of the polo-like kinase family with IC50 in the same range as for PI3K.

References: J Biol Chem. 1992 Feb 5; 267(4):2157-63.