A PAK1 inhibitor (Ki =3.7 nM); selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% (IC50s = 9-52 nM); inhibits phosphorylation of MEK (IC50 = 69 nM in EBC1 cells); reduces phosphorylation of MEK in tumors from an H292 NSCLC mouse xenograft model (10, 20, and 30 mg/kg); inhibits hERG channels by less than 50% at a concentration of 10 μM