Chemical Name: 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
Biological ActivityPotent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM). Displays 50 - 250-fold selectivity for FAK over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Cellular characterization of a novel focal adhesion kinase inhibitor.
Slack-Davis et al.
FAK-heterozygous mice display enhanced tumour angiogenesis.
Kostourou et al.
Citations for PF 573228
The citations listed below are publications that use Tocris products. Selected citations for PF 573228 include:
48 Citations: Showing 1 - 10
Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility.
Authors: Beerli Et al.
Nat Microbiol 2019;4:216
The increased adhesion of tumor cells to endothelial cells after irradiation can be reduced by FAK-inhibition.
Authors: Kouam Et al.
Radiat Oncol 2019;14:25
The protein tyrosine phosphatase Shp2 regulates oligodendrocyte differentiation and early myelination and contributes to timely remyelination.
Authors: Ahrendsen Et al.
J Neurosci 2018;38:787
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
Blood vitronectin is a major activator of LIF and IL-6 in the brain through integrin-FAK and uPAR signaling.
Authors: Keasey Et al.
J Cell Sci 2018;131
Multiparametric Analysis of Cell Shape Demonstrates that β-PIX Directly Couples YAP Activation to Extracellular Matrix Adhesion.
Authors: Sero and Bakal
Cell Syst 2017;4:84
Tenascin-C Is a Major Component of the Fibrogenic Niche in Kidney Fibrosis.
Authors: Fu Et al.
J Am Soc Nephrol 2017;28:785
Disruption of outer blood-retinal barrier by Toxoplasma gondii-infected monocytes is mediated by paracrinely activated FAK signaling
PLoS One 2017;12(4):e0175159
Imatinib and nilo. increase glioblastoma cell invasion via Abl-independent stimulation of p130Cas and FAK signalling.
Authors: Frolov Et al.
Sci Rep 2016;6:27378
Extracellular matrix stiffness dictates Wnt expression through integrin pathway.
Authors: Du Et al.
Sci Rep 2016;6:20395
Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices.
Authors: Nasrollahi and Pathak
PLoS One 2016;6:18831
Focal adhesion kinase is required for actin polymerization and remodeling of the cytoskeleton during sperm capacitation.
Authors: Roa-Espitia Et al.
Biol Open 2016;5:1189
LEFTY2 Controls Migration of Human Endometrial Cancer Cells via Focal Adhesion Kinase Activity (FAK) and miRNA-200a
Authors: Alowayed Et al.
Cell Physiol Biochem 2016;39:815
Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2.
Authors: Wang Et al.
Br J Pharmacol 2016;173:3342
Eosinophil peroxidase activates cells by HER2 receptor engagement and β1-integrin clustering with downstream MAPK cell signaling
Authors: Hennigan Et al.
Clinical Immunology 2016;171:1
Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
Authors: Rengarajan Et al.
Sci Rep 2016;12:e1005603
Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα.
Authors: Carrim Et al.
J Exp Med 2015;6:640
GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
Authors: Zhang Et al.
Redox Biol 2015;5:10468
Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
Authors: Gu Et al.
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.
IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
Authors: Cheng Et al.
Sci Rep 2015;212:513
WISP-2 in human gastric cancer and its potential metastatic suppressor role in gastric cancer cells mediated by JNK and PLC-γ pathways.
Authors: Ji Et al.
Br J Cancer 2015;113:921
Segmentation of Image Data from Complex Organotypic 3D Models of Cancer Tissues with Markov Random Fields.
Authors: Robinson Et al.
PLoS One 2015;10:e0143798
Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
Authors: Shih Et al.
J Biol Chem 2014;34:2438
The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis.
Authors: Flannagan Et al.
Mol Biol Cell 2014;25:1511
Essential function for PDLIM2 in cell polarization in three-dimensional cultures by feedback regulation of the β1-integrin-RhoA signaling axis.
Authors: Deevi Et al.
Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86.
Authors: Alao Et al.
BMC Cancer 2014;14:853
Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins.
Authors: Wrighton Et al.
PLoS Pathog 2014;111:18126
Periostin links mechanical strain to inflammation in abdominal aortic aneurysm.
Authors: Yamashita Et al.
J Neurosci 2013;8:e79753
Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
Authors: Wiel Et al.
Cell Death Dis 2013;4:e855
Reversal of myofibroblast differentiation by prostaglandin E(2).
Authors: Garrison Et al.
Mol Cancer Ther 2013;48:550
Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways.
Authors: Quint Et al.
PLoS One 2013;288:5398
Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis.
Authors: Barbelanne Et al.
Hum Mol Genet 2013;22:2482
Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor.
Authors: Chapman Et al.
J Immunol 2013;191:6208
Microdomain heterogeneity in 3D affects the mechanics of neonatal cardiac myocyte contraction.
Authors: Curtis Et al.
Biomech Model Mechanobiol 2013;12:95
Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
Authors: Keasey Et al.
Cell Commun Signal 2013;11:35
Contractile Activity Regulates Inducible Nitric Oxide Synthase Expression and NO(i) Production in Cardiomyocytes via a FAK-Dependent Signaling Pathway.
Authors: Chu Et al.
J Signal Transduct 2012;2012:473410
Focal adhesion kinase links mechanical force to skin fibrosis via inflammatory signaling.
Authors: Wong Et al.
Am J Respir Cell Mol Biol 2012;18:148
Integrin/Fak/Src-mediated regulation of cell survival and anoikis in human intestinal epithelial crypt cells: selective engagement and roles of PI3-K isoform complexes.
Authors: Beauséjour Et al.
Cooperation between c-Met and focal adhesion kinase family members in medulloblastoma and implications for therapy.
Authors: Guessous Et al.
Mol Cancer 2012;11:288
Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
Authors: Canonici Et al.
Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells.
Authors: Schrader Et al.
Biochem Biophys Res Commun 2011;53:1192
A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis.
Authors: Daley Et al.
Dev Dyn 2011;240:2069
β1 integrin mediates an alternative survival pathway in breast cancer cells resistant to lapa.
Authors: Huang Et al.
Breast Cancer Res 2011;13:R84
GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
Authors: Tu Et al.
J Neurosci 2010;30:749
DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway.
Authors: Ocak Et al.
tPA is a potent mitogen for renal interstitial fibroblasts: role of beta1 integrin/focal adhesion kinase signaling.
Authors: Hao Et al.
Am J Pathol 2010;177:1164
Characterization of a novel focal adhesion kinase inhibitor in human platelets.
Authors: Jones Et al.
Nat Med 2009;389:198
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Extracellular flux analysis (Seahorse experiments) of breast cancer cells. 5uM dose used for 48hrs
Effective at inhibiting FAK expression when used in 2D (monolayer) and 3D (spheroid/microtissue) cell culture