| Bioactivity | 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[1][2][3][4]. | ||||||||||||
| Target | IC50: 2 nM (FAK); 11 nM (PYK2).Kd: 445 nM (BRD4). | ||||||||||||
| Invitro | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PF-431396 相关抗体: Western Blot Analysis[3] Cell Line: | ||||||||||||
| In Vivo | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 717906-29-1 | ||||||||||||
| Formula | C22H21F3N6O3S | ||||||||||||
| Molar Mass | 506.50 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [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. [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. |
PF-431396
CAS: 717906-29-1 F: C22H21F3N6O3S W: 506.50
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with
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This product is for research use only, not for human use. We do not sell to patients.