PAK4-IN-2 is an exceptionally effective inhibitor of PAK4, exhibiting an IC 50 value of 2.7 nM. This compound is capable of arresting MV4-11 cells at the G0/G1 phase and inducing cell apoptosis. It holds significant potential in cancer research [1].

PAK4-IN-2 (compound 5n) (0-10 μM; 72 hours) exhibits cell growth inhibition potency in hematoma tumor MV4-11 and solid tumor cell line MDA-MB-231, shows less sensitivity in normal human renal epithelial cell 239 T cell [1]. PAK4-IN-2 (5-50 nM; 48 hours) causes a majority of cells in G0/G1 phase with decreasing S-phase populations [1]. PAK4-IN-2 (10-250 nM; 48 hours) induces apoptosis in a dose-dependent manner [1]. PAK4-IN-2 (50-800 nM; 24 hours) markedly reduces the expression levels of p-PAK4(Ser474) in concentration dependently [1]. Cell Proliferation Assay Cell Line: MV4-11, MDA-MB-231 and 293T [1] Concentration: 0-10 μM Incubation Time: 72 hours Result: Exhibited significant cell growth inhibition potency in hematoma tumor MV4-11 (IC 50 = 7.8 ± 2.8 nM), and moderate potent anti-proliferative effect in solid tumor cell line MDA-MB-231 (IC 50 = 825 ± 106 nM), less sensitivity in normal human renal epithelial cell 239 T cell (IC 50 > 10000 nM). Cell Cycle Analysis Cell Line: MV4-11 [1] Concentration: 5, 10 and 50 nM Incubation Time: 48 hours Result: Caused a majority of cells in G0/G1 phase with decreasing S-phase populations. Apoptosis Analysis Cell Line: MV4-11 [1] Concentration: 10, 50 and 250 nM Incubation Time: 48 hours Result: Induced apoptosis in a dose-dependent manner. Western Blot Analysis Cell Line: MV4-11 [1] Concentration: 50, 200 and 800 nM Incubation Time: 24 hours Result: Markedly reduced the expression levels of p-PAK4(Ser474) in concentration dependently.