NVS-PAK1-1 是一种有效的选择性变构 PAK1 抑制剂，IC50值为5 nM。

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases .

NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min).

1783816-74-9

C23H25ClF3N5O

479.93

DMSO:125 mg/mL (260.45 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years