[CAS NO. 1648863-90-4]  G-5555

G-5555 is a potent PAK1 inhibitor with a K _i of 3.7 nM. 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 Lck are 9, 11, 10, 20, 34, 43, 52 nM, respectively. In general, G-5555 demonstrates high selectivity for the group I PAKs. There is negligible activity for G-5555 against the hERG channel with IC ₅₀ more than 10 μM in a patch clamp assay ^[1] . G-5555 potently inhibits PAK2, with a K _i of 11 nM. In an array of 23 breast cancer cell lines, G-5555 has significantly greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.