Chemical Name: N-Methyl-N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Biological ActivityDual 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.
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.
Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis.
Buckbinder et al.
Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.
Han et al.
Emerging targets in osteoporosis disease modification.
Allen et al.
Citations for PF 431396
The citations listed below are publications that use Tocris products. Selected citations for PF 431396 include:
8 Citations: Showing 1 - 8
Unique-region phosphorylation targets LynA for rapid degradation, tuning its expression and signaling in myeloid cells.
Authors: Brian Et al.
CCL2/CCL5 secreted by the stroma induce IL-6/PYK2 dependent chemoresistance in ovarian cancer.
Authors: Pasquier Et al.
Mol Cancer 2018;17:47
Proline-rich tyrosine kinase 2 controls PI3-kinase activation downstream of the T cell antigen receptor in human T cells.
Authors: Chapman Et al.
Sci Rep 2015;97:285
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.
Authors: Kotla and Rao
J Biol Chem 2015;290:30306
IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
Authors: Cheng Et al.
BMC Neurosci 2015;212:513
HIV-1 Tat C phosphorylates VE-cadherin complex and increases human brain microvascular endothelial cell permeability.
Authors: Mishra and Singh
J Leukoc Biol 2014;15:80
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.
Authors: Kundumani-Sridharan Et al.
J Biol Chem 2013;288:15830
Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML.
Authors: Winter Et al.
Nat Chem Biol 2012;8:905
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