1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. PI5P4K

PI5P4K (PI5P4K)

PIP4K

PI5P4K/PIP4K(phosphatidylinositol 5-phosphate 4-kinase)是磷脂酰肌醇代谢中的关键酶,具有三种亚型:PI5P4KαPI5P4KβPI5P4Kγ,分别由基因 PIP4K2APIP4K2BPIP4K2C编码。这些激酶通过磷酸化磷脂酰肌醇5-磷酸(PI5P)生成磷脂酰肌醇4,5-二磷酸(PI(4,5)P2),对多种信号通路至关重要。PI5P4Ks 在细胞内膜上调节 PI(4,5)P2的水平,调控内吞等过程。PI5P与PI(4,5)P2之间的平衡对细胞应对压力的反应至关重要。

PI5P4Ks 参与关键的信号通路,特别是调节细胞生长的 Hippo 通路。Hippo 通路的激酶通过磷酸化抑制 PI5P4Ks 的活性。这两个重要的进化保守信号通路相关关联以调节多细胞生物的发展和人类疾病。在癌症生物学中,PI5P4Ks 表现出双重角色。例如,在前列腺癌中,较高的 PI5P4Kα 表达水平与较低的雄激素受体信号相关,提示其可能具有肿瘤抑制作用。相反,在其他情况下,它们可能通过增强压力条件下的生存通路促进肿瘤生长。它们活性的复杂平衡可能为癌症治疗提供通过操控这些信号通路的治疗靶点。

PI5P4K/PIP4K (phosphatidylinositol 5-phosphate 4-kinase) is a crucial enzyme in phosphoinositide metabolism, with three isoforms: PI5P4Kα, PI5P4Kβ, and PI5P4Kγ, encoded by the genes PIP4K2A, PIP4K2B, and PIP4K2C, respectively. These kinases phosphorylate phosphatidylinositol 5-phosphate (PI5P) to produce phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), which is vital for various signaling pathways. PI5P4Ks modulate the levels of PI(4,5)P2 at intracellular membranes, essential for processes like endocytosis. The balance between PI5P and PI(4,5)P2 is critical for cellular responses to stress.
PI5P4Ks are involved in key signaling pathways, particularly the Hippo pathway, which regulates cell growth. the Hippo pathway kinases phosphorylated and suppressed the activity of PI5P4Ks. These two important evolutionarily conserved signaling pathways are integrated to regulate metazoan development and human disease. In cancer biology, PI5P4Ks exhibit dual roles. For instance, in prostate cancer, higher expression levels of PI5P4Kα correlate with lower androgen receptor signaling, suggesting a potential tumor-suppressive role 3. Conversely, in other contexts, they may promote tumor growth by enhancing survival pathways under stress conditions. The intricate balance of their activity could provide therapeutic targets for cancer treatment by manipulating these signaling pathways.

PI5P4K 相关产品 (8):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-139868
    BAY-091 Inhibitor 99.55%
    BAY-091 是一种新型高效、高选择性的 PIP4K2A 激酶抑制剂。
    BAY-091
  • HY-101423
    NIH-12848 Inhibitor 99.84%
    NIH-12848 是推定的磷脂酰肌醇 5-磷酸4-激酶 γ (PI5P4Kγ) 抑制剂,IC50 值为 1 μM。
    NIH-12848
  • HY-139188
    CC260 Inhibitor 99.21%
    CC260 是一种选择性 PI5P4KαPI5P4Kβ 抑制剂,其 Ki 分别为 40 nM 和 30 nM。CC260 不抑制或弱抑制其他蛋白激酶,如 Plk1RSK2。CC260 可用于细胞能量代谢、糖尿病和癌症研究。
    CC260
  • HY-153531
    PI5P4Kα-IN-1 Inhibitor 98.49%
    PI5P4Kα-IN-1 (Compound 13) 是一种 PI5P4K 抑制剂 (IC50: PI5P4Kα 和 PI5P4Kβ 分别为 2 和 9.4 μM)。PI5P4Kα-IN-1 可用于癌症、代谢和免疫紊乱的研究。
    PI5P4Kα-IN-1
  • HY-152155
    ARUK2001607 Inhibitor 99.73%
    ARUK2001607 是一种选择性磷脂酰肌醇 5-磷酸 4-激酶 γ (PI5P4Kγ) 抑制剂,Kd 为 7.1 nM。ARUK2001607 显示出超过其他 >150 种激酶的高选择性。
    ARUK2001607
  • HY-153526
    PI5P4Ks-IN-2 Inhibitor 99.78%
    PI5P4Ks-IN-2 是磷脂酰肌醇 5-磷酸 4-激酶 PI5P4Kγ 的抑制剂。PI5P4Ks-IN-2 靶向 PI5P4K 亚型,pIC50 值分别 <4.3 (PI5P4Kα)、<4.6 (PI5P4Kβ)、6.2 (PI5P4Kγ)、0.32 (PI5P4Kγ+)。
    PI5P4Ks-IN-2
  • HY-145689
    PI5P4Ks-IN-1 Inhibitor
    PI5P4Ks-IN-1 (compound 7) 是一种活性化合物,对 PI5P4K α 或 β 同种型没有可检测到的抑制作用。
    PI5P4Ks-IN-1
  • HY-153532
    CVM-05-002 Inhibitor
    CVM-05-002 是 PI5P4K 抑制剂,其对PI5P4Kα 和PI5P4Kβ 的IC50 值分别为0.27 μM 和1.7 μM。
    CVM-05-002