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MW 479.93 g/mol, Purity >98%. NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1. It has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro assay. It is more than 50-fold more active against PAK1 than against PAK2. NVS-PAK1-1 is highly selective in a panel of 442 kinases. NVS-PAK1-1 potently inhibits PAK1 autophosphorylation in cell-based assays.

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Key facts

CAS number
1783816-74-9
Purity
> 98%
Form
Lyophilized
Molecular weight
479.93 g/mol
Molecular formula
C23H25ClF3N5O
Nature
Synthetic

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MW 479.93 g/mol, Purity >98%. NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1. It has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro assay. It is more than 50-fold more active against PAK1 than against PAK2. NVS-PAK1-1 is highly selective in a panel of 442 kinases. NVS-PAK1-1 potently inhibits PAK1 autophosphorylation in cell-based assays.

Key facts

Purity
> 98%
Solubility

Soluble in ethanol to 100 mM.

Soluble in DMSO to 100 mM.

Biological description

NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1. It has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro assay. It is more than 50-fold more active against PAK1 than against PAK2. NVS-PAK1-1 is highly selective in a panel of 442 kinases. NVS-PAK1-1 potently inhibits PAK1 autophosphorylation in cell-based assays.

Isomeric SMILES
O=C(NC(C)C)N4CC[C@H](NC1=NC3CC(F)CCC3N(CC(F)F)C2CCC(CL)CC12)C4
IUPAC name
(S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

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