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Wortmannin (KY 12420)

Cat. No. M2053
Wortmannin (KY 12420) Structure
Synonym:

SL-2052; KY-12420

Size Price Availability Quantity
2mg USD 54  USD54 In stock
5mg USD 72  USD72 In stock
10mg USD 135  USD135 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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
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.
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Wymann MP, et al. Mol Cell Biol. Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction.

[2] Powis G, et al. Cancer Res. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.

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  Catalog
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Keywords: Wortmannin (KY 12420), SL-2052; KY-12420 supplier, PI3K, inhibitors, activators


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