| Bioactivity | PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.)[1]. |
| Invitro | PAK4-IN-5 抑制细胞增殖，IC50分别为 1.87 μM (A-549)、1.56 μM (NCI-H1975)、1.21 μM (MDA-MB-231)、2.33 μM (SK-BR-3)、28.68 μM (Beas-2B)、26.68 μM (MCF-10A)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PAK4-IN-5 相关抗体: |
| Formula | C31H28ClN5O |
| Molar Mass | 522.04 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Hao S, et al. Design, synthesis and biological evaluation of novel benzimidazole-derived p21-activited kinase 4 (PAK4) inhibitors bearing a 4-(4-methylpiperazin-1-yl)phenyl scaffold as potential antitumor agents. Eur J Med Chem. 2024 Oct 17;280:116971. [2]. Meng FH. Design, synthesis and biological evaluation of novel benzimidazole-derived p21-activited kinase 4 (PAK4) inhibitors bearing a 4-(4-methylpiperazin-1-yl)phenyl scaffold as potential antitumor agents. Eur J Med Chem. 2024 Oct 17;280:116971. |