1. Signaling Pathways
  2. PI3K/Akt/mTOR
  3. PDK-1

PDK-1 (磷酸肌醇依赖性蛋白激酶-1)

PDK-1 (3-Phosphoinositide-dependent protein kinase 1), a member of the protein A, G and C (AGC) family of proteins, is a Ser/Thr protein kinase. PDK-1, is the pivotal node in the PI3K pathway, has a key role in insulin and growth-factor signalling through phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B.

PDK-1 is responsible for the regulation of cell proliferation and migration and it also has been found to play a key role in different cancers, pancreatic and breast cancer amongst others. Many cancer-driving mutations induce activation of PDK-1 targets including Akt, S6K (p70 ribosomal S6 kinase) and SGK. Thus, PDK1 is a critical activator of multiple pro-survival and oncogenic protein kinases, for which it has garnered considerable interest as an oncology drug target.

PDK-1 相关产品 (8):

目录号 产品名 作用方式 纯度
  • HY-10514
    BX795 Inhibitor 99.06%
    BX795 是一种有效的、选择性的 PDK1 抑制剂,IC50 值为 6 nM。同时,BX795 为有效、相对特异性的TBK1IKKɛ 的抑制剂,IC50 值分别为 6 和 41 nM。BX795 抑制 S6K1,Akt,PKCδ 和 GSK3β 的磷酸化。BX795 对 PKA,PKC,c-Kit,GSK3β 选择性较低。BX795 可调节自噬 (autophagy)。
  • HY-14981
    GSK2334470 Inhibitor 99.91%
    GSK2334470是高效特异性的 PDK1 抑制剂,IC50值为10 nM。
  • HY-N0047
    Polyphyllin I Inhibitor ≥98.0%
    Polyphyllin I 是一种从 Paris polyphylla 中提取的生物活性成分,具有很强的抗肿瘤活性。Polyphyllin I 是JNK 信号通路的激活剂,也是 PDK1/Akt/mTOR 信号传导的抑制剂。Polyphyllin I 诱导自噬,G2/M 期阻滞和细胞凋亡。
  • HY-14440
    MP7 Inhibitor 99.83%
    MP7 (PDK1 inhibitor) 是一种磷酸肌醇依赖性激酶-1 (PDK1) 抑制剂。
  • HY-11005
    BX-912 Inhibitor 99.53%
    BX-912 是一种直接的,选择性的,ATP 竞争性的 PDK1 抑制剂 (IC50=26 nM)。BX-912 阻断肿瘤细胞 PDK1/Akt 信号转导,抑制多种肿瘤细胞株的锚定依赖性生长或诱导凋亡。
  • HY-114645
    PDK1-IN-RS2 Inhibitor
    PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物,也是一种底物选择性 PDK1 抑制剂,Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。
  • HY-13842
    BX517 Inhibitor ≥98.0%
    BX517 是一种有效的,选择性的 PDK1 抑制剂,IC50 值为 6 nM。
  • HY-13856
    (R)-PS210 Inhibitor
    (R)-PS210 是 PS210 的 R 对映异构体 (化合物 4h-eutomer),是 PDK1 的底物选择性变构激活剂,AC50 值为 1.8 μM。(R)-PS210 靶向 PDK1 的 PIF 结合口袋。PIF: 蛋白激酶 C 相关激酶 2 (PRK2) 相互作用片段。
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