2. シグナル伝達
  3. Cell Cycle/DNA Damage
    Cytoskeleton
  4. PAK
  5. PAK4 Isoform

PAK4

PAK4 is a Cdc42-linked serine/threonine kinase that reorganizes the actin cytoskeleton and promotes filopodia formation[1]. Mechanistically, PAK4 cooperates with LIMK1 and cofilin to control cytoskeletal remodeling, linking upstream Rho GTPase signaling to cell-shape regulation[2]. This core function connects directly with cell proliferation and survival because PAK4 regulates cytoskeletal architecture, p21 expression, and cell-cycle progression[3]. In Wnt-related signaling, PAK4 shuttles between the cytoplasm and nucleus, phosphorylates β-catenin at Ser675, and increases β-catenin stability and TCF/LEF transcriptional activity[4]. In developmental models, PAK4 loss causes embryonic lethality and neuronal-development defects, supporting its use in cytoskeletal, developmental, and disease-relevant experimental systems[5]. In cancer models, PAK4 or PAK1 knockdown inhibits mutant KRAS colon cancer cell proliferation independently of RAF/MEK/ERK and PI3K/AKT signaling[6]. Compared with group I PAKs, PAK4 belongs to group II PAKs and uses an autoinhibitory pseudosubstrate mechanism, giving it distinct regulatory biology[7]. For experimental applications, PF-3758309 inhibits PAK4-dependent oncogenic signaling, whereas KPT-9274 inhibits PAK4 and blocks triple-negative breast cancer tumor growth in models[8][9].

References:

PAK4 関連製品 (17):

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-12793
    Padnarsertib Inhibitor 99.58%
    Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, 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-125035
    LCH-7749944 Inhibitor 99.68%
    LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.
  • HY-143490
    PAK4-IN-2 Inhibitor 99.42%
    PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer.
  • HY-183941
    SPU-106 Inhibitor
    SPU-106 is a p21 activated kinase 4 (PAK4) inhibitor with a target IC50 of 21.36 μM. SPU-106 selectively binds to the C-terminal kinase domain of PAK4 to inhibit its kinase activity. SPU-106 inhibits the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways. SPU-106 inhibits invasion of gastric cancer cells and lacks cytotoxicity against cancer cells. SPU-106 can be used for the research of gastric cancer.
  • HY-111103A
    CZh226 hydrochloride Inhibitor
    CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma.
  • HY-N8389
    Globulol Inhibitor 99.74%
    Globulol is a terpenoid metabolite and Antimicrobial agent. Globulol can be isolated from Alpinia oxyphylla Miq. Globulol binds to PAK4, reduces the expression level of PAK4 in cancer cells, decreases the phosphorylation of AKT, and downregulates the expressions of STAT3, phosphorylated STAT3, and PD-L1. Globulol promotes the secretion of CCL4 by cancer cells. Globulol reduces the viability and proliferation ability of cancer cells, induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and inhibits cancer cell migration and the integrity of 3D tumor spheres. Globulol enhances the relevant effects of anti-PD-1 agents in the cancer cell microenvironment. Globulol exhibits anticancer activity against liver cancer. Globulol inhibits the mycelial growth of phytopathogenic fungi and the growth of phytopathogenic bacteria. Globulol can be used in studies related to hepatocellular carcinoma.
  • HY-146681
    PAK1-IN-1 Inhibitor
    PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner.
  • 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-159897
    PAK4-IN-5 Inhibitor
    PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.).
  • 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-174247
    CPS-021 Degrader
    CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 has potent antimigratory and invasive activity and significantly suppresses the invasion and metastasis of tumor cells in A549-luc lung metastasis mice model. Pink: PAK4 ligand (HY-174822); Blue: CRBN ligase ligand (HY-10984); Black: linker
  • HY-130628
    PAK4-IN-1 Inhibitor
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions.
  • HY-181092
    PAK4-IN-7 Inhibitor
    PAK4-IN-7 is a selective ATP-competitive inhibitor of p21-activated kinase 4 (PAK4), with an IC50 of 1.88 μM. PAK4-IN-7 inhibits the proliferation of cancer cells. PAK4-IN-7 is applicable for research on tumors such as colorectal cancer and lung cancer.
  • HY-111103
    CZh226 Inhibitor
    CZh226 is a selective PAK4 inhibitor with an IC50 of 0.0111 μM and a Ki of 0.009 μM. CZh226 functionally inhibits PAK4 activity and reduces the phosphorylation level of downstream signaling molecules. CZh226 inhibits the migration and invasion of tumor cells. CZh226 is applicable to lung cancer-related research.
  • HY-117218
    KY-04045 Inhibitor
    KY-04045 is a PAK4 specific inhibitor (IC50=8.7 μM) that can be used for the development of anticancer drugs targeting PAK4.