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PIKfyve

PIKfyve

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.

PIKfyve related products

Structure Cat No. Product Name CAS No. Product Description
APY0201 V1558 APY0201 1232221-74-7 APY0201 (APY-0201; APY 0201) is a novel, potent and selectivePIKfyve inhibitor with potential anti-inflammatory activity.
AS2677131 V117646 AS2677131 2171502-44-4 AS2677131 is a potent, orally active PIKfyve inhibitor.
AS2795440 V120174 AS2795440 2171506-45-7 AS2795440 is a PIKfyve inhibitor.
PIKfyve-IN-1 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.
PIKfyve-IN-2 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.
TMX-4140 V118611 TMX-4140 2867519-51-3 TMX-4140 is a selective PIP4K2C inhibitor with a KD value of 7.2 nM for PIP4K2C, which is superior to its inhibitory activity against PIP4K2B.
WX8 V99637 WX8 232935-92-1 WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor with Kd values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively.
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