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Dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively). Promotes osteoblast recruitment and activity, and stimulates bone formation in ovariectomized rats.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 506.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||3.95 mL||19.74 mL||39.49 mL|
|2.5 mM||0.79 mL||3.95 mL||7.9 mL|
|5 mM||0.39 mL||1.97 mL||3.95 mL|
|25 mM||0.08 mL||0.39 mL||0.79 mL|
References are publications that support the biological activity of the product.
Buckbinder et al (2007) Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc.Natl.Acad.Sci.USA 104 10619 PMID: 17537919
Han et al (2009) Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J.Biol.Chem. 284 13193 PMID: 19244237
Allen et al (2010) Emerging targets in osteoporosis disease modification. J.Med.Chem. 53 4332 PMID: 20218623
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Keywords: PF 431396, PF 431396 supplier, PF431396, focal, adhesion, kinase, fak, proline-rich, tyrosine, 2, pyk2, inhibitors, inhibits, pfizer, Focal, Adhesion, Kinase, Other, Kinases, 4278, Tocris Bioscience
7 Citations for PF 431396
Citations are publications that use Tocris products. Selected citations for PF 431396 include:
Kundumani-Sridharan et al (2013) 12/15-Lipoxygenase mediates high-fat diet-induced endothelial tight junction disruption and monocyte transmigration: a new role for 15(S)-hydroxyeicosatetraenoic acid in endothelial cell dysfunction. J Biol Chem 288 15830 PMID: 23589307
Mishra and Singh (2014) HIV-1 Tat C phosphorylates VE-cadherin complex and increases human brain microvascular endothelial cell permeability. J Leukoc Biol 15 80 PMID: 24965120
Pasquier et al (2018) CCL2/CCL5 secreted by the stroma induce IL-6/PYK2 dependent chemoresistance in ovarian cancer. Mol Cancer 17 47 PMID: 29455640
Winter et al (2012) Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML. Nat Chem Biol 8 905 PMID: 23023260
Kotla and Rao (2015) Reactive Oxygen Species (ROS) Mediate p300-dependent STAT1 Protein Interaction with Peroxisome Proliferator-activated Receptor (PPAR)-γ in CD36 Protein Expression and Foam Cell Formation. J Biol Chem 290 30306 PMID: 26504087
Cheng et al (2015) IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function. BMC Neurosci 212 513 PMID: 25779634
Chapman et al (2015) Proline-rich tyrosine kinase 2 controls PI3-kinase activation downstream of the T cell antigen receptor in human T cells. Sci Rep 97 285 PMID: 25387834
Do you know of a great paper that uses PF 431396 from Tocris? Please let us know.
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