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Wortmannin

SL-2052

A Selective, Potent Inhibitor of PI3-Kinase

Cat #: W-400
Alternative Name SL-2052
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Penicillium fumiculosum (fungus).
    Source Natural
    MW: 428.4
    Purity: >98%
    Effective concentration 20-100 nM.
    Structure
    Chemical name (1S,6br,9aS,11R,11bR) 11-(Acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(metho xymethyl)-9a,11b-dimethyl-3Hfuro[4,3,2-de]indeno[4,5,- h]-2-h]-2-benzopyran-3,6,9-trione.
    Molecular formula C23H24O8.
    CAS No.: 19545-26-7
    Activity Wortmannin is a potent and specific inhibitor of PI3-kinase1. In PC12 cells treated with NGF, Wortmannin blocks the elongation of neurites2. At higher concentrations Wortmanin inhibits other kinases3,4.
    References-Activity
    1. Powis, G. et al. (1994) Cancer Res54, 2419.
    2. Kimura, K. et al. (1994) J. Biol. Chem. 269, 18961.
    3. Nakanishi, S. et al. (1992) J. Biol. Chem267, 2157.
    4. Ferby, I.M. et al. (1994) J. Biol. Chem. 269, 30485.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Wortmannin inhibits AKT phosphorylation via PI3-kinase in NIH-3T3 cells.
      Alomone Labs Wortmannin inhibits AKT phosphorylation via PI3-kinase in NIH-3T3 cells.
      Cells were preincubated for 30 min in different concentrations of LY 294002 (#L-300) or Wortmannin (#W-400) and then stimulated with PDGF (3 ng/ml) for 20 min. Cell proteins were resolved by SDS-PAGE and probed with (A) anti-phospho-AKT antibody, followed by stripping and reprobed with (B) anti-Akt antibody.
    References - Scientific background
    1. Powis, G. et al. (1994) Cancer Res54, 2419.
    2. Ui, M. et al. (1995) Trends Biochem. Sci20, 303.
    3. Hazeki, O. et al. (1996) J. Lipid Mediat. Cell Signal14, 259.
    4. Wymann, M. et al. (1994) Biochem. J298, 517.
    5. Bonser, R.W. et al. (1991) Br. J. Pharmacol103, 1237
    6. Arcaro, A. et al. (1993) Biochem. J296, 297.
    7. Kimura, K. et al. (1994) J. Biol. Chem269, 18961.
    8. Yano, H. et al. (1993) J. Biol. Chem268, 25846.
    9. Nakanishi, S. et al. (1992) J. Biol. Chem267, 2157.
    10. Ferby, I.M. et al. (1994) J. Biol. Chem269, 30485.
    Scientific background

    PI 3 Kinase is an enzyme implicated in growth factor signal transduction by associating with receptor and non-receptory tyrosine kinases. Wortmannin, a fungal metabolite (Penicillium fumiculosum), is a potent and specific inhibitor of phosphatidylinositol 3-kinase (PI-3K).1 It is highly cell-permeable, binds to the catalytic subunit of PI-3K and inhibits the enzyme activity in vitro and in vivo.2,3

    In purified preparations and cell-free cytosolic fractions it is active at 5 nM. In fibroblasts Wortmannin abolishes PDGF-mediated Inositol(3,4,5) P3 formation (IC50 = 5 nM).4 In guinea pig neutrophils it inhibits fMLP induced PIP3 and superoxide anion production (IC50 = 50 nM), and also phospholipase D activation.5,6 In PC12 cells treated with NGF, Wortmannin blocks the elongation of neurites.7 In rat basophilic leukemia (RBL-2H3) cells it inhibits IgE mediated histamine secretion.8 At higher concentrations Wortmanin inhibits other kinases such as myosin light chain kinase (IC50 = 200 nM)9 and MAP kinase activation (IC50 = 200-300 nM) induced by platelet activating factor.10

    Last update: 06/11/2022

    Wortmannin (#W-400) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Product citations
    1. Fernandez, J.A. et al. (2015) Invest. Ophtalmol. Vis. Sci. 56, 5125.
    2. Yu, C.H. et al. (2015) J. Immunol. 195, 3890.

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    Scientific Background

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