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

PAK

p21 activated kinases

PAK

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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:

PAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12005
    Fingolimod hydrochloride
    		Activator 99.95%
    Fingolimod (FTY720) hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride is also a pak1 activator and immunosuppressant.
    Fingolimod hydrochloride
  • HY-15027
    5-Aminosalicylic Acid
    		Inhibitor 99.82%
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
    5-Aminosalicylic Acid
  • HY-11063
    Fingolimod
    		Activator 99.97%
    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.
    Fingolimod
  • HY-13007
    PF-3758309
    		Inhibitor 99.84%
    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.
    PF-3758309
  • 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).
    IPA-3
  • HY-11063R
    Fingolimod (Standard)
    		Activator
    Fingolimod (Standard) is the analytical standard of Fingolimod. This product is intended for research and analytical applications. 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.
    Fingolimod (Standard)
  • 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.).
    PAK4-IN-5
  • HY-164488
    KT D606
    		Inhibitor
    KT D606 is an inhibitor of the PAK kinase family, with an IC50 value of 4 μM. KT D606 selectively blocks the proliferation of cancer cells transformed by oncogenic RAS mutants and can be used for research on RAS/PAK1-induced cancers.
    KT D606
  • HY-15542A
    FRAX597
    		Inhibitor 99.79%
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
    FRAX597
  • HY-100519
    NVS-PAK1-1
    		Inhibitor 99.50%
    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
    NVS-PAK1-1
  • HY-15323
    PRT062607 Hydrochloride
    		Inhibitor 98.07%
    PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.
    PRT062607 Hydrochloride
  • HY-15542B
    FRAX486
    		Inhibitor 98.01%
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
    FRAX486
  • 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.
    G-5555
  • HY-12793
    Padnarsertib
    		Inhibitor 99.86%
    Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively.
    Padnarsertib
  • HY-12632
    GNE 2861
    		Inhibitor 99.20%
    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.
    GNE 2861
  • HY-120940
    AZ13705339
    		Inhibitor 98.90%
    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.
    AZ13705339
  • HY-19538
    FRAX1036
    		Inhibitor 99.49%
    FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
    FRAX1036
  • HY-125035
    LCH-7749944
    		Inhibitor 99.36%
    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.
    LCH-7749944
  • 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.
    G-5555 hydrochloride
  • HY-139253
    MRIA9
    		Inhibitor 98.80%
    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.
    MRIA9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
PAK Isoform Comparison

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