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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pharmacological antagonists of FAK for 4 h before RNA or protein isolation. FAK antagonists were PF573228
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