Wortmannin (SL-2052) is a potent and specific PI3K inhibitor. The 50% inhibitory concentration for inhibition by wortmannin is 2 to 4 nM. Wortmannin inhibits polo-like kinase 1 (PLK1) with IC50 of 5.8 nM. Wortmannin 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.
|Cell lines||Human pancreatic adenocarcinoma cell lines PK1 and PK8|
|Preparation method||Drug Treatments. For flow cytometric analysis, cells were treated with the drug vehicle (≤1% DMSO) or 20 μM gemcitabine (2′,2′-diflurodeoxycytidine; Eli Lily & Co., Indianapolis, IN) for 48 h or with the same concentration of gemcitabine for the same duration followed by wortmannin (50–400 nM) or LY294002 (15–120 μM) for 4 h in the continuous presence of gemcitabine. The concentration and duration of gemcitabine treatment were chosen based on preliminary studies examining its effects on cell cycle inhibition and induction of apoptosis. For Western blotting, cells were treated with similar concentrations of wortmannin or LY294002 alone for 4 h or with gemcitabine (20 and 40μ M) alone for 48 h before harvest. Wortmannin and LY294002 were purchased from Biomol (Philadelphia, PA). All compounds were dissolved in DMSO at a stock concentration of 10 mM, stored at −20°C, and added to cell cultures at a final concentration of ≤1% DMSO, with appropriate solvent additions to control cultures. All experiments were performed in triplicate.|
|Incubation time||48 h|
|Animal models||mice bearing Orthotopic Model|
|Formulation||dissolved at 0.4 mg/ml in DMSO, and diluted with 0.9% NaCl before use.|
|Dosages||single bolus injections of 0.7 mg/kg|
|Administration||via the tail vein|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||APMIS.m (2017). Figure 7. wortmannin (Abmole Bioscience Inc. Houston, TX, USA)|
|Cell Lines||HeLa cells|
|Results||Moreover, cell pretreatment with wortmannin could reduce the expression level of p-PI3K, followed by slight augmentation in the inhibitory effects of 10-G on HeLa cells.|
J Agric Food Chem. 2017 Mar 15;65(10):2089-2099.
Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction.
Wymann MP, et al. Mol Cell Biol. 1996 Apr;16(4):1722-33. PMID: 8657148.
Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.
Powis G, et al. Cancer Res. 1994 May 1;54(9):2419-23. PMID: 8162590.
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