CZh226

CZh226 is a selective PAK4 inhibitor with an IC₅₀ of 0.0111 μM and a K_i of 0.009 μM. CZh226 functionally inhibits PAK4 activity and reduces the phosphorylation level of downstream signaling molecules. CZh226 inhibits the migration and invasion of tumor cells. CZh226 is applicable to lung cancer-related research^[1]. In Vitro:CZh226 (0.1-5.0 μM; 0-72 h) reduces the viability of human lung adenocarcinoma A549 cells, while exerts weak effects on PAK4-independent HEK-293 and NCI-H460 cells^[1].
CZh226 (0.5-10 μM; 24-48 h) inhibits the migration and invasion of human lung adenocarcinoma cell line A549 in a dose-dependent manner^[1].
CZh226 (0-10 μM; 24 h) inhibits the PAK4-dependent downstream signaling pathway in A549 cells in a dose-dependent manner^[1]. In Vivo:CZh226 (2 mg/kg; intravenous administration; single dose) exhibits moderate pharmacokinetic properties in male Sprague-Dawley rats, with a half-life of 1.46 h and an AUC_0-∞ of 472 ng·h/mL^[1].