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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $78 | 35 days |
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 |
Molecular Weight | 465.9 |
Formula | C22H23ClF3N5O |
Cas No. | 2250019-95-3 |
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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