PAK4-IN-2

PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> PAK

Signaling Pathways >> Cell Cycle/DNA Damage >> PAK

PAK3:2.7 nM (IC50)

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 (IC50 = 7.8 ± 2.8 nM), and moderate potent anti-proliferative effect in solid tumor cell line MDA-MB-231 (IC50 = 825 ± 106 nM), less sensitivity in normal human renal epithelial cell 239 T cell (IC50 > 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.

[1]. Wang C, Xia J, Lei Y, et al. Synthesis and biological evaluation of 7H-pyrrolo [2,3-d] pyrimidine derivatives as potential p21-activated kinase 4 (PAK4) inhibitors. Bioorg Med Chem. 2022;60:116700.