PF-4618433 是一种有效的、选择性的 PYK2 抑制剂，IC50 值为 637 nM。PF-4618433 可能适用于研究骨质疏松症，颅面和阑尾骨骼缺损以及靶向骨再生。
PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration[1][2].
PF-4618433 (0.1-1.0 μM; 7 days) promotes osteogenesis of hMSC cultures. PF-4618433 increases in both alkaline phosphatase (ALP) activity and mineralization in a dependent manner[1].PF-4618433 (0.1-0.3 μM; 24 hours) enhances osteoblast proliferation[2].PF-4618433 (0.0125-0.3 μM; 14 or 21 days) enhances calcium deposition at the concentrations of 0.1 and 0.3 μM[2].
参考文献:
[1]. Seungil H, 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): 13193-201.
[2]. Sumana P, et, al. A Pyk2 Inhibitor Incorporated Into a PEGDA-gelatin Hydrogel Promotes Osteoblast Activity and Mineral Deposition. Biomed Mater. 2019 Feb 27; 14(2): 025015.
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