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].
In Vitro, 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].
References:
[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.
In Vitro, 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].
References:
[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.