NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1, a serine-threonine kinase that is upregulated in many cancers. NVS-PAK1-1 has an IC
50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an
in vitro dephosphorylation assay. NVS-PAK1-1 showed good selectivity against 442 other kinases including PAK2. NVS-PAK1-1 has generally good physicochemical properties, but was metabolized by rat liver microsomes, so may not be useful for
in vivo work. For full characterization details, please visit the
NVS-PAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for protein targets, visit
sigma.com/sgc