PF-431396PF-431396
MedChemExpress (MCE)
HY-10460
717906-29-1
99.13%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
PF-431396 has a Kd value of 445 nM for BRD4[2]. PF-431396 appeares to selectively inhibit BCR-induced tyrosine phosphorylation of Pyk2 and FAK[3]. PF-431396 (2.5, 5 μM, 45 min) inhibits the phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs[3].
PF-431396 (10 or 30 mg/kg, orally) prevents bone loss induced by estrogen deficiency in rats primarily by stimulating bone formation, providing independent pharmacological confirmation for the function of PYK2 in regulating bone formation[4].
IC50: 2 nM (FAK)
11 nM (PYK2)[1]. Kd: 445 nM (BRD4)[1]. Cellular Effect Cell Line Type Value Description References
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[1]. Seungil Han, et al. Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem. 2009 May 8
284(19): 13193–13201. [Content Brief]
[2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [Content Brief]
[3]. Tse KW, et al. B cell receptor-induced phosphorylation of Pyk2 and focal adhesion kinase involves integrins and the Rap GTPases and is required for B cell spreading. J Biol Chem. 2009 Aug 21
284(34):22865-77. [Content Brief]
[4]. Leonard Buckbinder, et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc Natl Acad Sci U S A. 2007 Jun 19
104(25):10619-24. [Content Brief]