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].

PAK3:2.7 nM

PAK4-IN-2 (compound 5n) significantly inhibited cell growth in hematoma tumor MV4-11 and solid tumor MDA-MB-231 cell lines over 72 hours at concentrations of 0-10 μM, with reduced effects in normal renal epithelial cells (239T). At 5-50 nM for 48 hours, it predominantly arrested cells in the G0/G1 phase, reducing the S-phase population. PAK4-IN-2 also induced dose-dependent apoptosis in MV4-11 cells (10-250 nM for 48 hours) and significantly decreased p-PAK4(Ser474) levels in MV4-11 cells (50-800 nM for 24 hours). The compound exhibited strong anti-proliferative effects in MV4-11 cells (IC50 = 7.8 ± 2.8 nM), moderate effects in MDA-MB-231 cells (IC50 = 825 ± 106 nM), and minimal sensitivity in 239T cells (IC50 > 10000 nM).