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Home >> Signaling Pathways >> Cell Cycle/Checkpoint >> 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.

Targets for  PAK

Products for  PAK

  1. Cat.No. Product Name Information
  2. GC50370 AZ 13705339 Highly potent PAK1 and PAK2 inhibitor AZ 13705339 Chemical Structure
  3. GC66036 AZ13705339 hemihydrate 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. AZ13705339 hemihydrate Chemical Structure
  4. GC43666 Fingolimod Fingolimod is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb I. Fingolimod Chemical Structure
  5. GC14807 Fingolimod(FTY720) Fingolimod (FTY720) HCl (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod(FTY720) Chemical Structure
  6. GC10251 FRAX1036 p21-activated kinase I (PAK1) inhibitor FRAX1036 Chemical Structure
  7. GC16075 FRAX486 p21-activated kinase (PAK) inhibitor FRAX486 Chemical Structure
  8. GC12261 FRAX597 PAK inhibitor,potent and ATP-competitive FRAX597 Chemical Structure
  9. GC18720 G-5555 G-5555 is an inhibitor of p21-activated kinase 1 (PAK1; Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis. G-5555 Chemical Structure
  10. GC36095 G-5555 hydrochloride G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM. G-5555 hydrochloride Chemical Structure
  11. GC16225 IPA-3

    Non-ATP competitive Pak1 inhibitor

     IPA-3 Chemical Structure
  12. GC14615 KPT-9274 Orally acitve allosteric inhibitor of PAK4 KPT-9274 Chemical Structure
  13. GC39209 LCH-7749944 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 Chemical Structure
  14. GC16607 Mesalamine 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. Mesalamine Chemical Structure
  15. GC61043 Mesalamine impurity P Mesalamine impurity P is an impurity of Mesalamine. Mesalamine impurity P Chemical Structure
  16. GC62657 MRIA9 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 Chemical Structure
  17. GC32830 NVS-PAK1-1 An allosteric inhibitor of PAK1 NVS-PAK1-1 Chemical Structure
  18. GC44478 NVS-PAK1-C NVS-PAK1-C is a negative control for the allosteric PAK1 inhibitor NVS-PAK1-1. NVS-PAK1-C Chemical Structure
  19. GC33421 PAK-IN-1 PAK-IN-1 is a PAK inhibitor that displays group II selectivity. PAK-IN-1 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively. PAK-IN-1 Chemical Structure
  20. GC50314 PF 3758309 dihydrochloride Potent PAK4 inhibitor; orally available PF 3758309 dihydrochloride Chemical Structure
  21. GC17214 PF-3758309 An inhibitor of PAK4 PF-3758309 Chemical Structure

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