Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.

PI3K:3 nM, ATM:150 nM, DNA-PK:16 nM

METHODS: Human breast cancer cells MCF-7 were treated with Wortmannin (50-500 nM) for 24 h. Cell death was detected by Trypan blue exclusion assay.
RESULTS: Wortmannin induced cell death in MCF-7 cells in a concentration-dependent manner with an IC50 of 400 nM. [1]
METHODS: Human breast cancer cells MCF-7 were treated with Wortmannin (6.25-50 nM) for 24 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: Concentration-dependent reduction of p-Akt and NF-κB p65 expression was induced by Wortmannin. [2]

METHODS: To determine whether activation of the insulin pathway and brain enlargement were responsible for fatal seizures, Wortmannin (1.5 mg/kg) was administered orally to Pcmt1-/- mice once a day for twenty-two days.
RESULTS: Wortmannin reduced the average brain size of Pcmt1-/- mice to within 6% of that of controls and nearly doubled the lifespan of Pcmt1-/- mice, with a survival rate of 60% of the original population. [3]
METHODS: To investigate antitumor activity, Wortmannin (0.25-1 mg/kg) was injected intravenously three times a week for three weeks into SCID mice bearing the human breast cancer tumor MDA-MB-231.
RESULTS: Wortmannin significantly inhibited tumor metastasis and angiogenesis. [4]