1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. 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.

PAK 相关产品 (9):

Cat. No. Product Name Effect Purity
  • HY-15542A
    FRAX597 Inhibitor 99.19%
    FRAX597 是一种有效的 I型 P21激活激酶 (PAK)抑制剂,作用于 PAK123IC50 分别为 8,13 和 19 nM。
  • HY-13007
    PF-3758309 Inhibitor 98.41%
    PF-3758309 是一种有效的 PAK 抑制剂,能够抑制 PAK4 的活性,IC50 值为 1.3 nM。
  • HY-16291
    APTO-253 Inhibitor 99.16%
    APTO-253是一种新型小分子, 通过诱导Kruppel-样因子4 (KLF4)主转录因子基因表达, 发挥有效的抗肿瘤活性, 从而抑制细胞周期, 导致程序性细胞死亡。
  • HY-19635
    G-5555 Inhibitor 99.18%
    G-5555是一种有效的选择性PAK1 抑制剂 (Ki=3.7 nM)。
  • HY-12793
    KPT-9274 Inhibitor 99.28%
    KPT-9274是PAK的抑制剂, 来自专利专利WO 2015003166 A1,在MTT试验中测定的IC50值小于100nM。
  • HY-19635A
    G-5555 hydrochloride Inhibitor
    G-5555 hydrochloride是有效,选择性的PAK1抑制剂,Ki值为3.7 nM。
  • HY-15663
    IPA-3 Inhibitor >98.0%
    IPA-3 是一种选择性的,ATP 非竞争的 PAK1 抑制剂,IC50 值为 2.5 μM,对 PAKs 4-6 没有抑制作用。
  • HY-19538
    FRAX1036 Inhibitor >98.0%
    FRAX1036是新型ATP竞争性的PAK小分子抑制剂。
  • HY-15542B
    FRAX486 Inhibitor >98.0%
    FRAX486是group I PAKs有效选择性抑制剂,对PAK1、PAK2和PAK3的IC50值分别为8.25nM、39.5nM和55.3nM,对PAK4的抑制力弱(IC50=779nM)。