G-5555 hydrochloride is a potent and selective p21-activated kinase 1 ( PAK1 ) inhibitor with a K i of 3.7 nM.
Appearance:Solid
In Vitro:G-5555 shows excellent kinase selectivity and inhibits only eight out of the 235 kinases tested other than PAK1 with inhibition >70%: PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1. The IC 50 s of G-5555 against SIK2, PAK2, KHS1, MST4, YSK1, MST3 and L
In Vivo:G-5555 exhibits low blood clearance and an acceptable half-life. Good oral exposure (AUC=30 μM•h) and high oral bioavailability (F=80%) are achieved. In an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice, G-5555 inhibits phosphoryla
Biological Activity:G-5555 hydrochloride is a potent and selective p21-activated kinase 1 ( PAK1 ) inhibitor with a K i of 3.7 nM.
