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

PAK

PAKs (p21-activated kinases) are a family of six serine/threonine kinases that act as key effectors of RHO family GTPases in mammalian cells. PAKs are subdivided into two groups: group I (PAK1, PAK2, and PAK3) and group II (PAK4, PAK5, and PAK6), based on their domain architecture and regulation. Group I PAKs are activated by GTPases such as Cdc42, Rac, TC10, CHP, and Wrch-1, as well as in a GTPase-independent manner. Group II PAKs are generally not activated by Cdc42/Rac binding. PAK plays important roles in cytoskeletal organization, cellular morphogenesis, and survival, and members of this family have been implicated in many diseases including cancer, infectious diseases, and neurological disorders.

PAKs participate in various signaling networks. PAKs activate the MAPK pathway by phosphorylating Raf1 in addition to NF-κB. PAKs also phosphorylate a number of regulators of the cytoskeleton such as MLCK, LIMK, filamin A, ILK, merlin, and Arpc1b. In addition, PAKs regulate survival and apoptotic pathways through phosphorylation of its effectors such as DLC1 and BimL. On translocation to the nucleus, PAKs directly affect gene transcription. Several transcription factors and transcriptional co-regulators such as FKHR, SHARP, CTBP1 and SNAI1 are substrates to PAK1. PAKs also regulate cell cycle progression through phosphorylation of histone H3, Aurora A and PlK1.

PAK Isoform Specific Products:

  • PAK1

  • PAK2

  • PAK3

  • PAK4

  • PAK5

  • PAK6

PAK Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-12005
    Fingolimod hydrochloride
    Activator
    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
  • HY-13007
    PF-3758309
    Inhibitor 99.95%
    PF-3758309 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-15027
    5-Aminosalicylic Acid
    Inhibitor ≥98.0%
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-11063
    Fingolimod
    Activator 99.56%
    Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  • HY-15663
    IPA-3
    Inhibitor 99.43%
    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
  • HY-139253
    MRIA9
    Inhibitor
    MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively.
  • HY-15542A
    FRAX597
    Inhibitor 99.56%
    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 98.09%
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-100519
    NVS-PAK1-1
    Inhibitor ≥99.0%
    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
  • HY-19635
    G-5555
    Inhibitor ≥98.0%
    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-12632
    GNE 2861
    Inhibitor 99.47%
    GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
  • HY-19538
    FRAX1036
    Inhibitor ≥98.0%
    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 99.43%
    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-19635A
    G-5555 hydrochloride
    Inhibitor 98.78%
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-13007A
    PF-3758309 hydrochloride
    Inhibitor
    PF-3758309 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 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-131043
    NVS-PAK1-C
    Inhibitor
    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-131265
    Mesalamine impurity P
    Inhibitor
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Isoform Specific Products

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