PAK

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.

PAK 相关产品(24)

  • GC10251 structure
    GC10251FRAX1036
    CAS: 1432908-05-8
    纯度: >99.00%

    A selective PAK1 inhibitor

  • GC12261 structure
    GC12261FRAX597
    CAS: 1286739-19-2
    纯度: >98.00%

    A PAK1, PAK2, and PAK3 inhibitor

  • GC14615 structure
    GC14615KPT-9274
    CAS: 1643913-93-2

    Orally acitve allosteric inhibitor of PAK4

  • GC16075 structure
    GC16075FRAX486
    CAS: 1232030-35-1
    纯度: >98.00%

    A group I PAK inhibitor

  • GC16225 structure
    GC16225IPA-3
    CAS: 42521-82-4
    纯度: >99.00% / >98.00%

    An allosteric inhibitor of PAK1

  • GC17214 structure
    GC17214PF-3758309
    CAS: 898044-15-0
    纯度: >98.50%

    PF-3758309是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。

  • GC14807 structure
    GC14807Fingolimod (FTY720) HCl
    CAS: 162359-56-0
    纯度: >99.50% / >99.00%

    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)。

  • GC16607 structure
    GC16607Mesalamine
    CAS: 89-57-6
    纯度: >98.00%

    An NSAID and active metabolite of sulfasalazine, balsalazide, and olsalazine

  • GC18720 structure
    GC18720G-5555
    CAS: 1648863-90-4
    纯度: >99.00%

    A PAK1 inhibitor

  • GC32830 structure
    GC32830NVS-PAK1-1
    CAS: 1783816-74-9
    纯度: >99.00%

    An allosteric inhibitor of PAK1

  • GC33421 structure
    GC33421PAK-IN-1
    CAS: 1394121-05-1
    纯度: >99.00%

    A group 2 PAK inhibitor

  • GC36095 structure
    GC36095G-5555 hydrochloride
    纯度: >98.50%

    A PAK1 inhibitor

  • GC39209 structure
    GC39209LCH-7749944
    CAS: 796888-12-5
    纯度: >99.00%

    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.

  • GC43666 structure
    GC43666Fingolimod
    CAS: 162359-55-9
    纯度: >99.50% / >99.00%

    A fungal metabolite with immune modulating activities

  • GC44478 structure
    GC44478NVS-PAK1-C
    CAS: 2250019-95-3
    纯度: >98.00%

    A negative control for NVS-PAK1-1

  • GC50314 structure
    GC50314PF 3758309 dihydrochloride

    PF 3758309 dihydrochloride是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。

  • GC50370 structure
    GC50370AZ 13705339
    CAS: 2016806-57-6

    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。

  • GC61043 structure
    GC61043Mesalamine impurity P
    CAS: 887256-40-8

    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。

  • GC62657 structure
    GC62657MRIA9
    CAS: 2750707-05-0
    纯度: >98.00%

    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。

  • GC66036 structure
    GC66036AZ13705339 hemihydrate
    纯度: >99.00%

    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。

  • GC72148 structure
    GC72148st-Ht31 ammonium
    纯度: >95.00%

    st-Ht31 ammonium是蛋白激酶a (PKA)锚定的膜渗透性肽抑制剂。

  • GC72868 structure
    GC72868AZA197
    CAS: 1249398-09-1
    纯度: >98.00%

    AZA197是Cdc42的选择性小分子抑制剂。

  • GC73301 structure
    GC733015-Aminosalicylic acid-d3
    CAS: 1309283-32-6
    纯度: >99.00%

    5-Aminosalicylic acid-d3是氘标记的5-氨基水杨酸。

  • GC73424 structure
    GC73424PRT062607 acetate
    CAS: 1370261-98-5
    纯度: >99.00%

    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。