1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. PAK


PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases that are classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). Group I PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain, CD) and are activated by the binding of the active (that is, GTP-bound) forms of Rho GTPases, such as Cdc42 and Rac1. Group II PAKs have no auto-inhibitory domains and are not activated by active Rho GTPases. Because the deregulation of PAKs is closely associated with various human diseases,small-molecule inhibitors of these kinases have great potential as therapeutic agents. In addition, these compounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway.

PAKs are considered prime regulators of the actin cytoskeleton and motility. Due to their central role in actin remodelling and their ability to activate Matrix metalloproteinases (MMPs), Rho GTPases play an important role in tumor cell invasion and metastasis. The current evidence suggests the involvement of PAKs in motility, cell survival, anchorage-independent growth, angiogenesis, invasion, migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathological conditions including cancer.

PAK Isoform Specific Products:

  • PAK1

  • PAK2

  • PAK3

  • PAK4

  • PAK5

  • PAK6

PAK 相关产品 (16):

Cat. No. Product Name Effect Purity
  • HY-12005
    Fingolimod hydrochloride Activator 99.86%
    Fingolimod hydrochloride (FTY720) 是鞘氨醇1-磷酸 (S1P) 拮抗剂,在 K562 和 NK 细胞中的 IC50 为 0.033 nM。Fingolimod hydrochloride 还是一种 pak1 激活剂。
  • HY-13007
    PF-3758309 Inhibitor 99.95%
    PF-3758309 是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (Kd= 2.7 nM; Ki=18.7 nM)。PF-3758309 具有 PAK4 抑制剂的预期细胞功能:抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。
  • HY-15027
    5-Aminosalicylic Acid Inhibitor >98.0%
    5-Aminosalicylic acid (Mesalamine) 是一种特异性的 PPARγ 激动剂,还抑制 p21-激活激酶1 (PAK1) 和 NF-κB
  • HY-15663
    IPA-3 Inhibitor >98.0%
    IPA-3 是一种选择性的,ATP 非竞争的 PAK1 抑制剂,IC50 值为 2.5 μM,对 PAKs 4-6 没有抑制作用。
  • HY-11063
    Fingolimod Activator 99.81%
    Fingolimod (FTY720 free base) 是一种 1-磷酸鞘氨醇 (sphingosine 1-phosphateS1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50 为 0.033 nM。Fingolimod 还是一种 pak1 激活剂,免疫抑制剂。
  • HY-125035
    LCH-7749944 Inhibitor 99.43%
    LCH-7749944 (GNF-PF-2356) 是一种有效的 PAK4 抑制剂,IC50 为 14.93 μM。LCH-7749944通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖,并诱导凋亡 (apoptosis)。
  • HY-131265
    Mesalamine impurity P Inhibitor
    Mesalamine impurity P 是 Mesalamine (HY-15027) 的杂质。5-Aminosalicylic acid (Mesalamine) 是一种特异性的 PPARγ 激动剂,还抑制 p21-激活激酶 1 (PAK1) 和 NF-κB。
  • HY-13007B
    PF-3758309 dihydrochloride Inhibitor
    PF-3758309 dihydrochloride是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (Kd= 2.7 nM; Ki=18.7 nM)。PF-3758309 dihydrochloride 具有 PAK4 抑制剂的预期细胞功能:抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。
  • HY-15542B
    FRAX486 Inhibitor 98.09%
    FRAX486 是一种 PAK抑制剂,对 PAK1,PAK2 和 PAK3 的 IC50 值分别为 14,33 和 39 nM。
  • HY-15542A
    FRAX597 Inhibitor 99.56%
    FRAX597 是一种有效的 I型 P21激活激酶 (PAK)抑制剂,作用于 PAK123IC50 分别为 8,13 和 19 nM。
  • HY-19635
    G-5555 Inhibitor 99.18%
    G-5555 是有效 PAK1 抑制剂,对 PAK1 和 PAK2 的 Ki 值分别为 3.7 nM 和 11 nM。
  • HY-100519
    NVS-PAK1-1 Inhibitor >99.0%
    NVS-PAK1-1是有效,选择性的 PAK1 变构抑制剂,IC50值为5 nM。
  • HY-19538
    FRAX1036 Inhibitor 99.32%
    FRAX1036 是一种 PAK 抑制剂,对 PAK1,PAK2 和 PAK4 的 Ki 值分别为 23.3 nM,72.4 nM 和 2.4 μM。
  • HY-19635A
    G-5555 hydrochloride Inhibitor 98.78%
    G-5555 hydrochloride是有效,选择性的PAK1抑制剂,Ki值为3.7 nM。
  • HY-12632
    GNE 2861 Inhibitor 99.33%
    GNE 2861 是 PAK 的抑制剂,对 group II 具有选择性。GNE 2861 抑制 PAK4,PAK5 和 PAK6 的 IC50 值分别为7.5,36和126 nM。
  • HY-12793
    KPT-9274 Inhibitor 98.79%
    KPT-9274是有口服活性的 PAK4/烟酰胺磷酸核糖基转移酶 (Nampt) 抑制剂,IC50 值分别为小于 100 和 125 nM。
Isoform Specific Products

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Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.