The PIKFYVE gene in humans codes for the enzyme PIKfyve, a phosphoinositide kinase that contains the FYVE finger. PIKfyve's primary enzyme activity is the phosphorylation of PtdIns3P to PtdIns(3,5)P2. Both PtdIns(3,5)P2 and phosphatidylinositol 5-phosphate (PtdIns5P) are produced by PIKfyve activity. The large protein PIKfyve is expressed in various spliced forms and has several functional domains.The FYVE finger domain of PIKfyve is crucial for localizing the protein to the cytosolic leaflet of endosomes by directly interacting with membrane PtdIns(3)P. Endosome enlargement and cytoplasmic vacuolation are brought on by decreased PtdIns(3,5)P2 synthesis, which is impaired by dominant-interfering mutants, siRNA-mediated ablation, or pharmacological inhibition of the PIKfyve enzyme. As a result, PIKfyve participates in various endosome dynamics through the production of PtdIns(3,5)P2, which has an impact on a number of trafficking pathways that originate from or pass through the endosomal system on their way to the trans-Golgi network or later compartments along the endocytic pathway.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V1558 | APY0201 | 1232221-74-7 | APY0201 (APY-0201; APY 0201) is a novel, potent and selectivePIKfyve inhibitor with potential anti-inflammatory activity. | |
V69245 | PIKfyve-IN-1 | 2857982-26-2 | PIKfyve-IN-1 is a potent and cell-active chemical probe that can inhibit phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) with IC50 of 6.9 nM. | |
V69243 | PIKfyve-IN-2 | 2245319-25-7 | PIKfyve-IN-2 is a potent PIKfyve kinase inhibitor that may be utilized in cancer and autoimmune disease study. |