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PAK(p21激活激酶)

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.

Products for  PAK

  1. Cat.No. 产品名称 Information
  2. GC66036 AZ13705339 hemihydrate AZ13705339 hemihydrate 是一种高效且具有选择性的 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。AZ13705339 hemihydrate 对 PAK1 和 PAK2 具有结合亲和力,Kd 分别为 0.28 nM 和 0.32 nM。AZ13705339 hemihydrate 可用于癌症研究。
  3. GC62657 MRIA9 MRIA9 是 ATP 竞争性的、pan-SIK 和 PAK2/3 抑制剂,其对 SIK1、SIK2 和 SIK3 的 IC50 值分别为 516 nM, 180 nM 和 127 nM。
  4. GC61043 Mesalamine impurity P MesalamineimpurityP是Mesalamine的杂质。5-Aminosalicylicacid(Mesalamine)是一种特异性的 PPARγ 激动剂,还抑制p21-激活激酶1(PAK1)和 NF-κB。
  5. GC50370 AZ 13705339 AZ 13705339 是一种高效的选择性 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。 AZ 13705339 与 PAK1 和 PAK2 具有结合亲和力,Kds 分别为 0.28 nM 和 0.32 nM。 AZ 13705339 可用于癌症研究。
  6. GC50314 PF 3758309 dihydrochloride An inhibitor of PAK4
  7. GC39209 LCH-7749944 LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
  8. GC36095 G-5555 hydrochloride A PAK1 inhibitor
  9. GC44478 NVS-PAK1-C A negative control for NVS-PAK1-1
  10. GC43666 Fingolimod A fungal metabolite with immune modulating activities
  11. GC33421 PAK-IN-1 A group 2 PAK inhibitor
  12. GC32830 NVS-PAK1-1 An allosteric inhibitor of PAK1
  13. GC18720 G-5555 A PAK1 inhibitor
  14. GC10251 FRAX1036 A selective PAK1 inhibitor
  15. GC16075 FRAX486 A group I PAK inhibitor
  16. GC14615 KPT-9274 Orally acitve allosteric inhibitor of PAK4
  17. GC16225 IPA-3 An allosteric inhibitor of PAK1
  18. GC12261 FRAX597 A PAK1, PAK2, and PAK3 inhibitor
  19. GC16607 Mesalamine An NSAID and active metabolite of sulfasalazine, balsalazide, and olsalazine
  20. GC14807 Fingolimod (FTY720) HCl

    Fingolimod (FTY720), an immunosuppressant agent, usually used in the treatment of multiple sclerosis, also has anticancer actions and can act as an HDACi (Histone deacetylase inhibitors)[1].

  21. GC17214 PF-3758309 An inhibitor of PAK4

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