pikfyve

YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

Apilimod mesylate (STA 5326 mesylate) is a potent IL-12 IL-23 inhibitor.

PIKfyve-IN-4 (Compound 40) is an orally active and selective phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) inhibitor, with an IC50 of 0.60 nM, and demonstrates good systemic tolerability.

PIKfyve-IN-2 is a potent inhibitor of the PIKfyve kinase, with potential applications in cancer and autoimmune disorder research (Figure 4).

PIKfyve-IN-1 is a cell-active and highly potent chemical probe that can be used for the PIKfyve research in virology. PIKfyve-IN-1 inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) (IC 50 = 6.9 nM)[1].

antibody against human PIKfyve

Vacuolin-1 is a cell-permeable inhibitor of Ca2+ dependent fusion of lysosomes to the cell membrane. It acts by inhibiting release of lysosomal content.vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation

WX8 (Ro 91-4714) is an ATP-competitive inhibitor of PIKFYVE, displaying Kd values of 0.9 nM for PIKFYVE and 340 nM for PIP4K2C. This compound inhibits lysosomal fission without affecting homotypic lysosome fusion. WX8 (Ro 91-4714) is applicable in research on autophagy-dependent cancers.

Apilimod 2HCl (STA 5326 2HCl) is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation, IL-1β secretion, and cellular pyroptosis, and is used in the study of amyotrophic lateral sclerosis.

UNI418 is a dual inhibitor targeting PIKfyve and PIP5K1C, exhibiting antiviral activity against SARS-CoV-2 (EC50=1.4 μM). It inhibits the endocytosis of the virus mediated by ACE2 by suppressing PIP5K1C (IC50=60.1 nM; Kd=61 nM). Additionally, UNI418 impedes the entry of SARS-CoV-2 into host cells by inhibiting the proteolytic activation regulated by PIKfyve (Kd=0.78 nM).

DC-SX029 is a potent inhibitor of SNX10 protein-protein interaction (PPI) with an estimated K D constant of approximately 0.935 μM as measured by surface plasmon resonance (SPR). It blocks the SNX10-PIKfyve interaction, leading to decreased TBK1 c-Rel signaling activation, without affecting SNX10 protein levels. DC-SX029 shows potential for inflammatory bowel disease (IBD) research [1].

APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3, 5)P2.

PIK5-12d is a PROTAC PIKfyve degrader with antitumor activity that induces massive cytoplasmic vacuolization and blocks autophagic flow. PIK5-12d inhibits the value-added of cancer cells and can be used in the study of prostate cancer.

MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].