681676
Wortmannin
≥95% (HPLC), PI3K inhibitor, liquid
Synonym(s):
InSolution Wortmannin, MLCK Inhibitor II
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About This Item
Empirical Formula (Hill Notation):
C23H24O8
Molecular Weight:
428.43
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Product Name
Wortmannin, InSolution, ≥95%, fungal metabolite that acts as a selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase)
Quality Level
description
Merck USA index - 14, 10053
assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
shipped in
wet ice
storage temp.
−20°C
General description
Wortmannin is a fungal metabolite known for its potent and selective inhibitory effects onphosphatidylinositol 3-kinase (PI 3-kinase). It serves as a cell-permeable and irreversible inhibitor, demonstrating an IC50 of 5 nM in both purified preparations and cytosolic fractions. When fibroblasts are preincubated with wortmannin, it effectively abolishes the formation of Ins (3,4,5) P3 mediated byplatelet-derived growth factor (PDGF). Wortmannin blocks the catalytic activity of PI 3-kinase without interfering with upstream signaling events, making it a valuable tool for studying PI 3-kinase pathways. Additionally, it inhibits the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor′s tyrosinekinase activity. Wortmannin inhibits MAP kinase activation induced by platelet-activating factor in guinea pig neutrophils at concentrations ranging from 0.2 to 0.3 µM. It also demonstrates the ability to inhibit osteoclastic bone resorption. While it primarily targets PI 3-kinase, wortmannin can inhibit other kinases, such as myosin light chain kinase, with an IC50 of 200 nM, and PI 4-kinase at concentrations 100-fold higher than those required for PI3-kinase inhibition. Wortmannin also blocks phospholipase D activity. This steroid metabolite can inhibit human non-small cell lung cancer (NSCLC) both in vitro and in vivo. It acts as an effective radio sensitizer, increasing the sensitivity of NSCLC cells to ionizing radiation.
Application
Wortmannin has been used:
- to treat the cells transfected withspecific vectors to investigate its role as an autophagy inhibitor
- as a classical autophagy inhibitor to evaluate its effects on autophagic flux in non-small cell lung cancer (NSCLC) cells, specifically H460 cells
- in inhibitor treatment experiments to inhibit autophagy and also used along with bafilomycin A1 to inhibit lysosomal degradation
Packaging
Packaged under inert gas
Physical form
A 10 mM (1 mg/233 µl) solution of Wortmannin (Cat. No. 681675) in DMSO.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Inhalation - Acute Tox. 4 Oral
Storage Class
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Certificates of Analysis (COA)
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