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.
Front Pharmacol. 2023 Jun 29;14:1181319.
Liang-Ge-San: a classic traditional Chinese medicine formula, attenuates acute inflammation via targeting GSK3β
Wortmannin (KY 12420) purchased from AbMole
Platelets. 2023 Feb 22;2173505.
Alantolactone induces platelet apoptosis by activating the Akt pathway
Wortmannin (KY 12420) purchased from AbMole
Front Pharmacol. 2021 Sep 23;12:749930.
Carbamazepine Induces Platelet Apoptosis and Thrombocytopenia Through Protein Kinase A
Wortmannin (KY 12420) purchased from AbMole
J Infect Dis. 2018 May 8.
Tumor Necrosis Factor-α Is Required for Mast Cell-Mediated Host Immunity Against Cutaneous Staphylococcus aureus Infection.
Wortmannin (KY 12420) purchased from AbMole
J Agric Food Chem. 2017 Mar 15;65(10):2089-2099.
10-Gingerol, a Phytochemical Derivative from “Tongling White Ginger”, Inhibits Cervical Cancer: Insights into the Molecular Mechanism and Inhibitory Targets
Wortmannin (KY 12420) purchased from AbMole
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Source | J Infect Dis (2018). Figure 7. Wortmannin (Abmole Bioscience) |
| Method | Western blotting | |
| Cell Lines | mast cells | |
| Concentrations | 10 μM | |
| Incubation Time | 30 minutes | |
| Results | The S. aureus-induced production of TNF-α and CRAMP was significantly reduced by pretreatment with the specific PI3K inhibitor Wortmannin or the specific NF-κB inhibitor PDTC |
. figure 7.jpg) |
Source | APMIS.m (2017). Figure 7. wortmannin (Abmole Bioscience Inc. Houston, TX, USA) |
| Method | Western blot | |
| Cell Lines | HeLa cells | |
| Concentrations | ||
| Incubation Time | ||
| 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. |
| Cell Experiment | |
|---|---|
| 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. |
| Concentrations | 50–400 nM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| 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 |
| Molecular Weight | 428.43 |
| Formula | C23H24O8 |
| CAS Number | 19545-26-7 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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| PI3Kα-IN-13
PI3Kα-IN-13 is a PI3Kα inhibitor (IC50: 2.5 nM). |
| FD2056
FD2056 is a potent and orally active PI3K inhibitor. |
| Acetyl-Exenatide
Acetyl-Exenatideyes is an acetylated derivative of Exenatide. |
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