2. シグナル伝達
  3. Cell Cycle/DNA Damage
    Cytoskeleton
  4. PAK
  5. PAK2 Isoform

PAK2

PAK2 (p21-activated kinase 2) is a ubiquitously expressed serine/threonine kinase of the group I PAK family that functions as a major downstream effector of the small GTPases CDC42 and RAC1, linking Rho GTPase signaling to cytoskeletal remodeling and nuclear signaling pathways[1][2]. PAK2 activation is mediated through release of autoinhibition within its regulatory domain, followed by autophosphorylation and kinase activation, enabling regulation of cell adhesion, actin dynamics, cell division, apoptosis, and intracellular signal transduction[2]. Mechanistically, PAK2 participates in multiple signaling networks and can modulate transforming growth factor-β (TGF-β) responses by restricting R-Smad phosphorylation and transcriptional activity, highlighting its role in signal integration and cellular homeostasis[3]. In disease-related contexts, aberrant PAK signaling has been associated with cancer progression, cell survival, migration, and cytoskeletal reorganization, making PAK family members important subjects in experimental oncology research[4]. Compared with the closely related isoforms PAK1 and PAK3, PAK2 is distinguished by its ubiquitous expression pattern and its requirement for embryonic development, whereas PAK1 shows more restricted adult tissue expression and PAK3 is predominantly expressed in the brain[2]. Notably, PAK2 is the only PAK family member directly activated by caspase-3-mediated proteolytic cleavage, generating a constitutively active kinase fragment that contributes to apoptotic signaling and cellular stress responses. For experimental applications, small-molecule group I PAK inhibitors such as FRAX597 have been widely used to suppress PAK activity and investigate PAK-dependent signaling mechanisms in tumor and cell biology models[2].

PAK2 関連製品 (15):

製品番号 製品名 製品効果 純度
  • HY-13007
    PF-3758309 Inhibitor 99.79%
    PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-15542A
    FRAX597 Inhibitor 99.36%
    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-15542B
    FRAX486 Inhibitor 98.10%
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-19635
    G-5555 Inhibitor 99.88%
    G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
  • HY-19538
    FRAX1036 Inhibitor 98.88%
    FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
  • HY-182357
    PAK1-IN-3 Inhibitor
    PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM, an IC50 of 20 nM against PAK2, and an IC50 of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels.
  • HY-120940
    AZ13705339 Inhibitor 98.57%
    AZ13705339 is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 can be used in the research of cancers.
  • HY-19635A
    G-5555 hydrochloride Inhibitor 98.26%
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-171034
    PQA-18 Inhibitor 99.62%
    PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice.
  • HY-131043
    NVS-PAK1-C Inhibitor 99.2%
    NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM).
  • HY-120940A
    AZ13705339 hemihydrate Inhibitor 99.77%
    AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 hemihydrate can be used in the research of cancers.
  • HY-13007A
    PF-3758309 hydrochloride Inhibitor
    PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-13007B
    PF-3758309 dihydrochloride Inhibitor
    PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-116917
    G-9791 Inhibitor
    G-9791, a poyridone side chain analogue, is a potent PAK inhibitor with Ki values of 0.95 nM and 2.0 nM for PAK1 and PAK2, respectively.
  • HY-146786
    ZMF-10 Inhibitor
    ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer.
製品番号 製品名 / Synonyms Application Reactivity