1. PI3K/Akt/mTOR
  2. PIKfyve

PIKfyve

PIKfyve, a FYVE finger-containing phosphoinositide kinase, is an enzyme that in humans is encoded by the PIKFYVE gene. The principal enzymatic activity of PIKfyve is to phosphorylate PtdIns3P to PtdIns(3,5)P2. PIKfyve activity is responsible for the production of both PtdIns(3,5)P2 and phosphatidylinositol 5-phosphate (PtdIns5P). PIKfyve is a large protein, containing a number of functional domains and expressed in several spliced forms. By directly binding membrane PtdIns(3)P, the FYVE finger domain of PIKfyve is essential in localizing the protein to the cytosolic leaflet of endosomes. Impaired PIKfyve enzymatic activity by dominant-interfering mutants, siRNA- mediated ablation or pharmacological inhibition causes endosome enlargement and cytoplasmic vacuolation due to impaired PtdIns(3,5)P2 synthesis. Thus, via PtdIns(3,5)P2 production, PIKfyve participates in several aspects of endosome dynamics, thereby affecting a number of trafficking pathways that emanate from or traverse the endosomal system en route to the trans-Golgi network or later compartments along the endocytic pathway.

PIKfyve 相关产品 (2):

Cat. No. Product Name Effect Purity
  • HY-13228
    YM-201636 Inhibitor 98.88%
    YM-201636 是高效选择性的 PIKfyve 抑制剂,IC50 值为 33 nM。YM-201636 也抑制 p110α,IC50 为 3.3 μM。
  • HY-15982
    APY0201 Inhibitor 98.56%
    APY0201 是一种有效的 PIKfyve 抑制剂,抑制 PtdIns3P 转化为PtdIns(3,5)P2IC50 为 5.2 nM。 APY0201 还抑制 IL-12/23 产生。