Wortmannin, 1 mg

A small-molecule, covalent inhibitor of phosphatidylinositol 3-kinase (PI3K) and polo-like kinase (PLK) pathways, with cytotoxic effects on cancer cells, supplied by STEMCELL Technologies. The fungal metabolite binds class I, II, and III PI3K enzymes, with reported IC50 values for class II enzymes of 5, 50, and 450 nM in Drosophila, mouse, and human, respectively. The compound also inhibits PLK1 and PLK3 with IC50 values of 24 and 49 nM, respectively, and at higher concentrations can affect other kinases including mTOR, DNA-PKcs, PI4K, MLCK, and MAPK.

Published applications include cytotoxic activity against human tumor cell lines in vitro and anti-tumor activity in mouse xenograft models of C3H mammary carcinoma and BxPC-3 pancreatic carcinoma. The compound is a crystalline solid with chemical formula C23H24O8, molecular weight 428.4 g/mol, CAS number 19545-26-7, and reported purity of ≥ 98%. Approximate solubility is 0.1 mg/mL in 1:8 DMSO:PBS (pH 7.2), 0.15 mg/mL in ethanol, and 14 mg/mL in DMF and DMSO. Stock solutions may be prepared in DMSO (≤ 30 mM) or absolute ethanol (≤ 0.3 mM) and the product is stable at -20°C, protected from light.

According to the manufacturer's Safety Data Sheet, the substance is classified as Acute Toxicity Category 1 (oral, inhalation) and Category 2 (skin), and is fatal if swallowed, in contact with skin, or inhaled. An intraperitoneal LD50 of 18 mg/kg has been reported in mouse. The toxicological properties have not been fully evaluated, and the compound has been investigated as a reproductive effector. Identified target organs include the heart, and exposure may cause gastric or myocardial hemorrhage.