NVS-PAK1-1|PAK1 inhibitor|cas 1783816-74-9
DC Chemicals, Website: www.dcchemicals.com
Product Name: NVS-PAK1-1|Cas Number: 1783816-74-9| Catalog Number: DC10473|Other Nmaes: NVS-PAK1-1，NVS-PAK11，NVS-PAK1 1
NVS-PAK1-1 potently inhibits autophosphorylation of PAK1 (S144) at 0.25 µM in the Su86.86 cell line and MEK S289 phosphorylation with an IC50 = 0.21 in Su86.86 cells in which PAK2 is downregulated.
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.
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