Catalog Number: 4278
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 Activity
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.
Technical Data
  • M.Wt:
    506.5
  • Formula:
    C22H21F3N6O3S
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    717906-29-1
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis.
    Buckbinder et al.
    Proc.Natl.Acad.Sci.USA, 2007;104:10619
  2. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.
    Han et al.
    J.Biol.Chem., 2009;284:13193
  3. Emerging targets in osteoporosis disease modification.
    Allen et al.
    J.Med.Chem., 2010;53:4332
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PF 431396 include:

4 Citations: Showing 1 - 4
Filter your results:

  1. 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
  2. IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
    Authors: Cheng Et al.
    BMC Neurosci 2015;212:513
  3. 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
  4. 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

Have you used PF 431396?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

or select another batch: 

Feedback

Customer Information