FAK Inhibitor 14
Chemical Name: 1,2,4,5-Benzenetetramine tetrahydrochloride
Biological Activity
FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. FAK Inhibitor 14 prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. FAK Inhibitor 14 exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth.
Golubovskaya et al.
J.Med.Chem., 2008;51:7405 -
A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer.
Hochwald et al.
Cell Cycle, 2009;8:2435
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Citations for FAK Inhibitor 14
The citations listed below are publications that use Tocris products. Selected citations for FAK Inhibitor 14 include:
23 Citations: Showing 1 - 10
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Focal adhesion kinase confers pro-migratory and antiapoptotic properties and is a potential therapeutic target in Ewing sarcoma.
Authors: Konrad Et al.
Mol Oncol 2020;14:248-260
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Vitronectin from brain pericytes promotes adult forebrain neurogenesis by stimulating CNTF.
Authors: Theo Et al.
Exp Neurol 2019;312:20-32
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Fibroblast activation protein-α promotes the growth and migration of lung cancer cells via the PI3K and sonic hedgehog pathways.
Authors: Jia Et al.
Int J Mol Med 2018;41:275
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Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin.
Authors: Bastounis Et al.
Mol Biol Cell 2018;29:1571
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Plectin protects podocytes from adriamycin-induced apoptosis and F-actin cytoskeletal disruption through the integrin α6β4/FAK/p38 MAPK pathway.
Authors: Ni Et al.
J Cell Mol Med 2018;22:5450
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Homodimers of vanillin and apocynin decrease the metastatic potential of human cancer cells by inhibiting the FAK/PI3K/Akt signaling pathway.
Authors: Jantaree Et al.
J.Agric.Food Chem. 2017;65:2299
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Netrin-1 suppresses the MEK/ERK pathway and ITGB4 in pancreatic cancer.
Authors: An Et al.
Oncotarget 2016;7:24719
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Integrin-FAK signaling rapidly and potently promotes mitochondrial function through STAT3.
Authors: Visavadiya
Cell Communication and Signaling 2016;14:32
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Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
Authors: Rengarajan Et al.
PLoS One 2016;12:e1005603
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Inhibition of STAT3, FAK and Src mediated signaling reduces cancer stem cell load, tumorigenic potential and metastasis in breast cancer.
Authors: Thakur Et al.
Sci Rep 2015;5:10194
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Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells.
Authors: Webber Et al.
Oncoscience 2015;2:765
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RECK-Mediated β1-Integrin Regulation by TGF-β1 Is Critical for Wound Contraction in Mice.
Authors: Gutiérrez Et al.
J Neurosci 2015;10:e0135005
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Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment.
Authors: McLane and Ligon
Biophys J 2015;109:249
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Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
Authors: Shih Et al.
Auton Neurosci 2014;34:2438
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OE and tamox. induce cell migration through GPR30 and activation of focal adhesion kinase (FAK) in endometrial cancers with low or without nuclear estrogen receptor α (ERα).
Authors: Tsai Et al.
PLoS One 2013;8:e72999
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ERBB4 confers metastatic capacity in Ewing sarcoma.
Authors: Mendoza-Naranjo Et al.
EMBO Mol Med 2013;5:1019
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Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
Authors: Wiel Et al.
Cell Death Dis 2013;4:e855
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CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
Authors: Malenczyk Et al.
J Biol Chem 2013;288:32685
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Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis.
Authors: Barbelanne Et al.
Hum Mol Genet 2013;22:2482
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Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
Authors: Keasey Et al.
Cell Commun Signal 2013;11:35
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Contractile equilibration of single cells to step changes in extracellular stiffness.
Authors: Daniel A Et al.
Biophys J 2012;102:443-51
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Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells.
Authors: Afrikanova Et al.
J Biol Chem 2011;286:36042
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GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
Authors: Tu Et al.
J Neurosci 2010;30:749
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