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NVS-PAK1-C

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NVS-PAK1-C

Catalog No. T35928Cas No. 2250019-95-3

NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].

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Pack Size	Price	Availability	Quantity
1 mg	$78	35 days

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Product Introduction

Bioactivity

Description	NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].
In vitro	NVS-PAK1-1 potently inhibits PAK1 (S144) autophosphorylation at 0.25 μM in the Su86.86 cell line and MEK S289 phosphorylation with an IC 50 =0.21 μM in Su86.86 cells in which PAK2 is downregulated [1].
Alias	NVS-PAK1-C

Chemical Properties

Molecular Weight	465.9
Formula	C22H23ClF3N5O
Cas No.	2250019-95-3

Storage & Solubility Information

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility Information	DMSO: 50 mg/mL DMF: 50 mg/mL Ethanol: 20 mg/mL DMSO:PBS(pH7.2) (1:1): 0.5 mg/mL

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Keywords

NVSPAK1CNVS PAK1 CNVS-PAK-1-C