Wortmannin

貨號 Cat. No.: W-400
規格 Size: 10 x 0.25 mg 1mg 5mg 5x5mg

Description

Wortmannin

A Selective, Potent Inhibitor of PI 3-Kinase

Product#:

W-400

Sizes:

10 x 0.25 mg

1 mg

5 mg

5 x 5 mg

(Penicillium fumiculosum), is a potent and specific inhibitor of phosphatidylinositol 3-kinase (PI-3K).¹It 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

M.W.:

428.4

CAS No.:

[19545-26-7]

Structure:

Purity:

>98%

Bioassay:

The biological activity was tested to confirm the ability of Wortmannin to inhibit PI 3 - Kinase activity.

NIH/3T3 cells were preincubated for 30 min in different concentrations

of Wortmannin, and then stimulated with PDGF (3ng/ml) for 20 min.

The cell extracts were blotted and probed with (A) Phosphorylated- AKT

antibody, followed by stripping and re-probing with (B) antibody to Akt protein.

References:

1.	Powis, G. et al. (1994) Cancer Res. 54, 2419.
2.	Ui, M. et al. (1995) Trends Biochem. Sci. 20, 303.
3.	Hazeki, O. et al. (1996) J. Lipid Mediat. Cell Signal. 14, 259.
4.	Wymann, M. et al. (1994) Biochem. J. 298 Pt 3, 517.
5.	Bonser, R.W. et al. (1991) Br. J. Pharmacol. 103, 1237.
6.	Arcaro, A. et al. (1993) Biochem. J. 296 ( Pt 2), 297.
7.	Kimura, K. et al. (1994) J. Biol. Chem. 269, 18961.
8.	Yano, H. et al. (1993) J. Biol. Chem. 268, 25846.
9.	Nakanishi, S. et al. (1992) J. Biol. Chem. 267, 2157.
10.	Ferby, I.M. et al. (1994) J. Biol. Chem. 269, 30485.

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

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