PAKs (p21 activated kinases) are members of a family of enzymes. They serve as targets for the small GTP binding proteins CDC42 and Rac and have been implicated in a wide range of biological activities. Members include PAK1 (regulating cell motility and morphology),PAK2 (possibly playing a role in apoptosis),PAK3 (possibly for dendritic development and for the rapid cytoskeletal reorganization in dendritic spines associated with synaptic plasticity),PAK4 (a mediator of filopodia formation),PAK5 (a mediator of filopodia formation) and PAK6 (involved in cytoskeleton rearrangement).
  • FRAX 486 EI1147

    FRAX 486是活性的 PAK 抑制剂, 可透血脑屏障的,口服有效。

  • IPA-3 EY1503

    IPA-3是非ATP竞争的PAK1选择性抑制剂,IC50为2.5 μM,对于II型 PAKs (PAKs 4-6)无抑制活性。

  • PF-3758309 EY0420

    PF-3758309, a potent ATP-competitive inhibitor of PAK1 and PAK4, displays broad anti-tumor activity in cellular proliferation and apoptosis. PF-3758309是PAK4抑制剂,IC50为1.3 nM,能抑制HCT116,A549,M24met和别的肿瘤外植体模型。

  • FRAX597 EY1277


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