PAK1-IN-1

PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner[1].

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> PAK

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

PAK1:9.8 nM (IC50)

PAK4:>10 μM (IC50)

PAK1-IN-1 (compound 30l) (0-10 µM) shows selectivity with IC50s of 0.01, >10 µM for PAK1 and PAK4, respectively[1]. Cell Proliferation Assay[1] Cell Line: MDA-MB-231, HCT-116 cells Concentration: 1 µM Incubation Time: 72 h Result: Showed antiproliferative activity against MDA-MB-231and HCT-116 cells with inhibition of 6.31% and 8.73%, respectively. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5, 5, 10, 20 µM Incubation Time: 1, 24 h Result: Decreased the expression of activated PAK1 (PAKp-Ser144) and Snail in a dose-dependent manner.

[1]. Zhang M, et al. Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities. Eur J Med Chem. 2020 Oct 1;203:112517.