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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. GC73424 PRT062607 acetate

    P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate

    PRT062607 acetate是一种口服Syk抑制剂(IC50: 1 nM),可抑制炎症和诱导细胞凋亡。
  3. GC73301 5-Aminosalicylic acid-d3

    Mesalamine-d3; 5-ASA-d3; Mesalazine-d3

    5-Aminosalicylic acid-d3是氘标记的5-氨基水杨酸。
  4. GC72868 AZA197 AZA197是Cdc42的选择性小分子抑制剂。
  5. GC72148 st-Ht31 ammonium st-Ht31 ammonium是蛋白激酶a (PKA)锚定的膜渗透性肽抑制剂。
  6. 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。
  7. 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。
  8. GC61043 Mesalamine impurity P

    美沙拉嗪EP杂质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。
  9. 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。
  10. GC50314 PF 3758309 dihydrochloride

    PF-03758309 dihydrochloride

    An inhibitor of PAK4
  11. GC39209 LCH-7749944

    GNF-PF-2356

    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.
  12. GC36095 G-5555 hydrochloride A PAK1 inhibitor
  13. GC44478 NVS-PAK1-C A negative control for NVS-PAK1-1
  14. GC43666 Fingolimod

    芬戈莫德; FTY720 free base

    A fungal metabolite with immune modulating activities
  15. GC33421 PAK-IN-1 A group 2 PAK inhibitor
  16. GC32830 NVS-PAK1-1 An allosteric inhibitor of PAK1
  17. GC18720 G-5555 A PAK1 inhibitor
  18. GC10251 FRAX1036 A selective PAK1 inhibitor
  19. GC16075 FRAX486 A group I PAK inhibitor
  20. GC14615 KPT-9274 Orally acitve allosteric inhibitor of PAK4
  21. GC16225 IPA-3 An allosteric inhibitor of PAK1
  22. GC12261 FRAX597 A PAK1, PAK2, and PAK3 inhibitor
  23. GC16607 Mesalamine

    5-氨基水杨酸; Mesalamine; 5-ASA; Mesalazine

    An NSAID and active metabolite of sulfasalazine, balsalazide, and olsalazine
  24. GC14807 Fingolimod (FTY720) HCl

    盐酸芬戈莫德; FTY720

    芬戈莫德(FTY720)是一种免疫抑制剂,通常用于治疗多发性硬化症,也有抗癌作用,可以作为HDACi(组蛋白脱乙酰酶抑制剂)。
  25. GC17214 PF-3758309

    PF 3758309; PF3758309

    An inhibitor of PAK4

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