1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. PAK

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 Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-15542A
    FRAX597 Inhibitor 99.19%
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
  • HY-13007
    PF-3758309 Inhibitor 98.41%
    PF-3758309 is an inhbitor of PAK with IC50 of 1.3 nM for PAK4.
  • HY-16291
    APTO-253 Inhibitor 99.16%
    APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death
  • HY-19635
    G-5555 Inhibitor 99.18%
    G-5555 is a selective PAK1 Inhibitor (Ki=3.7 nM).
  • HY-12793
    KPT-9274 Inhibitor 99.28%
    KPT-9274 is an inhibitor of p21-activated kinase (PAK) extracted from patent WO 2015003166 A1; has an IC50 of less than 100 nM in MTT assay.
  • HY-19635A
    G-5555 hydrochloride Inhibitor
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-15663
    IPA-3 Inhibitor >98.0%
    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).
  • HY-19538
    FRAX1036 Inhibitor >98.0%
    FRAX1036 is a novel ATP-competitive small molecule inhibitor of group I p21-activated Kinases (PAKs).
  • HY-15542B
    FRAX486 Inhibitor 98.08%
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s between 10-100 nM for PAK1-3.