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NVS-PAK1-1

Chemical Structure : NVS-PAK1-1

CAS No.: 1783816-74-9

NVS-PAK1-1 (PAK1 inhibitor)

Catalog No.: PC-49534Not For Human Use, Lab Use Only.

NVS-PAK1-1 is a potent, selective and allosteric inhibitor of PAK1 with IC50 of 5 nM, potently inhibits PAK1 phosphorylation in vitro and in vivo.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NVS-PAK1-1 is a potent, selective and allosteric inhibitor of PAK1 with IC50 of 5 nM, potently inhibits PAK1 phosphorylation in vitro and in vivo.
NVS-PAK1-1 is almost 100× more selective for PAK1 than PAK2.
NVS-PAK1-1 potently inhibited PAK1 autophosphorylation in MS02 cells, and reduced the proliferation of MS02 and HEI-193 cells with an IC50 of 4.7 and 6.2 μM, respectively.
NVS PAK1-1 (30 mg/kg) reduces the average dorsal root ganglia (DRG) size in Nf2-cKO mice.

Physicochemical Properties

M.Wt 479.932
Formula C23H25ClF3N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide

References

1. Chudi O Ndubaku, et al. ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6.

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