AG 82 - CAS 118409-58-8 - Calbiochem

A cell-permeable, reversible, and competitive inhibitor of substrate binding on protein tyrosine kinases. Inhibits epidermal growth factor receptor tyrosine kinase (IC₅₀ = 3 µM) and the GTPase activity of transducin (IC₅₀ = 7 µM). Blocks the induction of inducible nitric oxide synthase in glial cells. Induces apoptosis in human leukemic cell lines. Also reported to inhibit guanylyl cyclase.

A cell-permeable, reversible, and competitive inhibitor of substrate binding on protein tyrosine kinases. Inhibits epidermal growth factor receptor tyrosine kinase (IC₅₀ = 3 µM) and the GTPase activity of transducin (IC₅₀ = 7 µM). Inhibits neuromedin B-induced phosphorylation of p125^FAK (focal adhesion kinase). Blocks the induction of inducible nitric oxide synthase in glial cells. Induces apoptosis in human leukemic cell lines.

Cell permeable: yes

Primary Target
epidermal growth factor receptor tyrosine kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 3 µM against epidermal growth factor receptor tyrosine kinase

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

Jaleel, M., et al. 2004. Biochemistry43, 8247.
Tsuda, T., et al. 1997. Biochemistry 36, 16328.
Wolbring, G., et al. 1994. J. Biol. Chem. 269, 22470.
Bergamaschi, G., et al. 1993. Leukemia7, 2012.
Piontek, M., et al. 1993. Anticancer Res.13, 2119.
Bilder, G.E., et al. 1991. Am. J. Physiol. 260, C721.
Gazit, A., et al. 1989. J. Med. Chem. 32, 2344.
Yaish, P., et al. 1988. Science242, 933.

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

Toxicity: Standard Handling (A)