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Datasheet of NVS-PAK1-1
Description: 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. NVSPAK1-1 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.
Chemical Information Catalog
DC10473
Purity of current batch:
>98%
Molecular Weight (MW)
479.93
Molecular Formula
C23H25ClF3N5O
CAS No.
1783816-74-9
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.