Biochem/physiol Actions

Primary Targetepidermal growth factor receptor autophosphorylation

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 40 µM against epidermal growth factor receptor autophosphorylation; 10 µM against GTPase activity of transducin

General description

A cell-permeable, reversible, substrate competitive protein tyrosine kinase inhibitor. Inhibits epidermal growth factor receptor autophosphorylation (IC₅₀ = 40 µM) and the GTPase activity of transducin (IC₅₀ = 10 µM). Inhibits aldosterone secretion in response to angiotensin II. Suppresses the activation of MAP kinases by cholecystokinin in pancreatic acini. Also reported to inhibit guanylyl cyclase.

A broad-spectrum protein tyrosine kinase inhibitor. Inhibits epidermal growth factor receptor autophosphorylation (IC₅₀ = 40 µM) and the GTPase activity of transducin (IC₅₀ = 10 µM). Inhibits aldosterone secretion in response to Angiotensin II (Cat. No. 05-23-0101). Suppresses the activation of MAP kinases by cholecystokinin in pancreatic acini.

Legal Information

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

Other Notes

Jaleel, M., et al. 2004. Biochemistry43, 8247.Kapas, S., et al. 1995. Biochem. J. 305, 433.Seger, R., et al. 1995. J. Biol. Chem.270, 28325.Williams, J.A. 1994. Am. J. Physiol.267, G401.Geissler, J.F., et al. 1990. J. Biol. Chem.265, 22255.Levitzki, A. 1990. Biochem. Pharmacol.40, 913.Gazit, A., et al. 1989. J. Med. Chem. 32, 2344.Lyall, R.M., et al. 1989. J. Biol. Chem. 264, 14503.

Packaging

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)