Merck, 658395-5MG, AG 18

General description
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.
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.
Biochem/physiol Actions
Cell permeable: no
Primary Target
epidermal growth factor receptor autophosphorylation
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 40 µM against epidermal growth factor receptor autophosphorylation; 10 µM against GTPase activity of transducin
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)