PF-3758309(PF3758309) PAK4抑制剂|CAS 898044-15-0（53872ES）

PF-3758309 (PF3758309)是可口服的、可逆的、ATP竞争性PAK4抑制剂，IC₅₀为1.3 nM，K_d为2.7 nM，K_i为18.7 nM。PAK4在肌动蛋白细胞骨架重组中有重要作用。PF-3758309抑制PAK4底物(GEF-H1)磷酸化和PAK4诱导的锚定非依赖性细胞生长，诱导凋亡，具有潜在抗肿瘤活性。

参考文献

[1] Murray BW, et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51.

[2] Ryu BJ, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389(1-2):69-77.

冰袋运输。粉末直接保存于-20℃，有效期3年。建议分装后-20℃干燥保存，避免反复冻融。