Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 8 µM, 10 µM, 300 nM, 200 nM against cyclooxygenase, 5-lipoxygenase, 12-lipoxygenase, and 15-lipoxygenase , respectively, in whole cells

Primary TargetPLA₂

Cell permeable: yes

General description

Cell-permeable. Inhibits arachidonic acid uptake and arachidonic acid specific and nonspecific acyl-CoA synthesis. Inhibits phospholipase A₂ (PLA₂) and cytochrome P-450. Inhibits cyclooxygenase (ID₅₀ = 8 µM), 5-lipoxygenase (ID₅₀ = 10 µM), 12-lipoxygenase (ID₅₀ = 300 nM), and 15-lipoxygenase (ID₅₀ = 200 nM) in whole cells. A potent modulator of Ca²⁺ entry into cells. Stimulates luteinizing hormone release from cultured pituitary cells.

Cell permeable. Inhibits arachidonic acid uptake and the activities of arachidonic acid specific and non-specific acyl-CoA synthetases. Inhibits phospholipase A₂ (PLA₂) and cytochrome P-450. Inhibits cyclooxygenase (ID₅₀ = 8 µM), 5-lipoxygenase (ID₅₀ = 10 µM), 12-lipoxygenase (ID₅₀ = 300 nM), and 15-lipoxygenase (ID₅₀ = 200 nM) in whole cells. Also acts as a potent modulator of Ca²⁺ entry into cells. Blocks monocyte binding in minimally-oxidized LDL in endothelial cells. Stimulates luteinizing hormone release from cultured pituitary cells.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Honda, H.M., et al. 1999. Arterioscler. Thromb. Vasc. Biol.19, 680.Ekokoski, E., and Tornquist, K. 1994. Biochim. Biophys. Acta 1223, 274.Ondrey, F., et al. 1989. Cancer Res.49, 1138.Kuhn, H., et al. 1984. Eur. J. Biochem.139, 577.

Packaging

20 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)