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Merck

681676

Wortmannin

≥95% (HPLC), PI3K inhibitor, liquid

동의어(들):

InSolution Wortmannin, MLCK Inhibitor II

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C23H24O8
Molecular Weight:
428.43
UNSPSC Code:
12352200
NACRES:
NA.77
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제품 이름

Wortmannin, InSolution, ≥95%, fungal metabolite that acts as a selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase)

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

Quality Level

Disclaimer

Toxicity: Harmful (C)

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

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

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.

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Acute Tox. 4 Inhalation - Acute Tox. 4 Oral

저장 등급

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)


시험 성적서(COA)

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문서

Discover definitions and uses for irreversible inhibitors including the types of irreversible inhibitors: suicide inhibitors, heavy metal inhibitors, and time-dependent inhibitors.

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