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FAK inhibitor 14 is a direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 with an IC50 value of about 1 μM.1 There is no known significant effect on the activity of a range of other kinases. FAK inhibitor 14 promotes cell detachment and inhibits cell adhesion of cells in culture.1 Moreover, it blocks tumor growth in vivo.1,2,3 FAK inhibitor 14 has also been used to demonstrate a role for FAK in the regulation of aortic stiffness.4
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1. A small molecule inhibitor, 1,2,4,5-
2. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8(15), 2435-2443 (2009).
3. Inhibition of focal adhesion kinase decreases tumor growth in human neuroblastoma. Cell Cycle 9(5), 1005-1015 (2010).
4. The focal adhesion: A regulated component of aortic stiffness. PLoS One 8(4), (2013).