Cat. No. 3239
Chemical Name: 3,4-Dihydro-6-[[4-[[[3-(methylsulfo
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.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Kostourou et al (2013) FAK-heterozygous mice display enhanced tumour angiogenesis. Nat.Commun. 5 2020. PMID: 23799510.
Slack-Davis et al (2007) Cellular characterization of a novel focal adhesion kinase inhibitor. J.Biol.Chem. 282 14845. PMID: 17395594.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for PF 573228 include:
Alowayed et al (2016) LEFTY2 Controls Migration of Human Endometrial Cancer Cells via Focal Adhesion Kinase Activity (FAK) and miRNA-200a Cell Physiol Biochem 39 815. PMID: 27497669.
Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069. PMID: 25621765.
Webber et al (2015) Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells. Oncoscience 2 765. PMID: 26501082.
Alao et al (2014) Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer 14 853. PMID: 25409876.
Flannagan et al (2014) The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis. Mol Biol Cell 25 1511. PMID: 24623723.
Chapman et al (2013) Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor. J Immunol 191 6208. PMID: 24227778.
Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35. PMID: 23693126.
Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855. PMID: 24113189.
Beauséjour et al (2012) 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. Apoptosis 17 566. PMID: 22402981.
Chu et al (2012) Contractile Activity Regulates Inducible Nitric Oxide Synthase Expression and NO(i) Production in Cardiomyocytes via a FAK-Dependent Signaling Pathway. J Signal Transduct 2012 473410. PMID: 22900166.
Daley et al (2011) A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis. Dev Dyn 240 2069. PMID: 22016182.
Hao et al (2010) tPA is a potent mitogen for renal interstitial fibroblasts: role of beta1 integrin/focal adhesion kinase signaling. Am J Pathol 177 1164. PMID: 20639453.
Ocak et al (2010) DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway. Oncogene 29 6331. PMID: 20802517.
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749. PMID: 20071540.
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Keywords: PF 573228, supplier, Potent, selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, PF573228, Tocris Bioscience, Focal Adhesion Kinase Inhibitor products
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