Description
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-
dependent cell proliferation. AG-
183 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC
50 value of 0.8 μM in the human epidermoid carcinoma cell line A431.
Uses
Tyrphostin 51 is a potent inhibitor of EGFRK activity showing mixed competitive inhibition with ATP and substrate1-3..
Definition
ChEBI: 2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile is a benzenetriol.
References
[1] gazit a, yaish p, gilon c, et al. tyrphostins i: synthesis and biological activity of protein tyrosine kinase inhibitors[j]. journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[2] hubbard s r, till j h. protein tyrosine kinase structure and function[j]. annual review of biochemistry, 2000, 69(1): 373-398.
