Chemical Name: 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate
Biological ActivityApilimod dimesylate is a potent and selective PIKfyve inhibitor (IC50 = 14 nM). Exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. Apilimod dimesylate reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. Also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells. Inhibits production of IL-12 and IL-23. In motor neurons derived from patients with amyotrophic lateral sclerosis (ALS) Apilimod dimesylate promotes exocytosis of neurotoxic proteins and in mouse ALS models, the compound reduces pathology and prolongs survival. Anti-inflammatory. Water-soluble.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor.
Wada et al.
PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling.
Cai et al.
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing.
Riva et al.
Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV.
Ou et al.
Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma.
Gayle et al.
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