2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
NVS-PAK1-1 is a potent, allosteric PAK1 inhibitor. It is about 60-fold selective over PAK2. It is highly selective over other kinases in the kinome. It has a submicromolar IC50 in a PAK1 autophosphorylation assay. These features make it a useful tool to assess the impact of PAK1 inhibition in a cellular context. More data would need to be collected, but poor microsomal stability (rat) suggests the compound may not be suitable for use in model organisms (in vivo applications).NVS-PAK1-1 has an IC50 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.
