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

PDK-1 (磷酸肌醇依赖性蛋白激酶-1)

3-Phosphoinositide-dependent protein kinase 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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135773
    CRTh2 antagonist 3 Activator
    CRTh2 antagonist 3 是有效的 Th2 细胞上表达的趋化受体同源分子 (CRTh2) 拮抗剂。CRTh2 antagonist 3 增强了PDK1 对短肽底物的活性,EC50 为 2 μM,Kd 为 8.4 μM。CRTh2 antagonist 3 有用于心血管炎症的潜力。
    CRTh2 antagonist 3
  • HY-146978
    LDHA/PDKs-IN-2 Inhibitor
    LDHA/PDKs-IN-2 (compound 20k) 是一种有效的 PDKs 和 LDHA 双重抑制剂,IC50s 分别为 1.6 和 0.7 μM。LDHA/PDKs-IN-2 减少 A549 细胞增殖,EC50 为 15.7 μM,减少乳酸形成,增加耗氧量。LDHA/PDKs-IN-2 具有研究癌症疾病的潜力。
    LDHA/PDKs-IN-2
  • HY-149275
    PKM2/PDK1-IN-1 Inhibitor
    PKM2/PDK1-IN-1 是一种紫草素硫醚衍生物,是 PKM2/PDK1 的双重抑制剂。 PKM2/PDK1-IN-1抑制NSCLC细胞的增殖,并诱导细胞凋亡 (apoptosis)。 PKM2/PDK1-IN-1 诱导细胞间 ROS 产生,调节凋亡蛋白,参与线粒体和死亡受体通路。
    PKM2/PDK1-IN-1
  • HY-117885
    PF-5177624 Inhibitor
    PF-5177624 是一种特异性强效的 PDK1 抑制剂,PDK1 是 PI3K/AKT 信号通路中的关键酶,在乳腺癌中经常失调。PDK1 在 T308 和其他底物处磷酸化 AKT,激活对肿瘤进展很重要的下游信号通路。PF-5177624 阻断 IGF-1 刺激的 PDK1 活性和下游 AKTp70S6K 磷酸化,减少乳腺癌细胞的细胞增殖和转化。
    PF-5177624
目录号 产品名 / 同用名 应用 反应物种