NVS-PAK1-C 是一种有效的、ATP 竞争的特异性变构PAK1抑制剂探针。NVS-PAK1-C可抑制去磷酸化的 PAK1(IC50= 5 nM) 和磷酸化的 PAK1(IC50= 6 nM)。NVS-PAK1-C 也可以抑制去磷酸化的 PAK2 (IC50=270 nM) 和磷酸化的 PAK2 (IC50=720 nM)。

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].

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].

2250019-95-3

C22H23ClF3N5O

465.9

NVS-PAK1-C;NVS-PAK1-C

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