Apilimod dimesylate

Biological Activity

Apilimod 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor.
   Wada et al.
   Blood, 2007;109:1156
2. 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.
   Chem.Biol., 2013;20:912
3. Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing.
   Riva et al.
   Nature, 2020;
4. Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV.
   Ou et al.
   Nat.Commun., 2020;11:1620
5. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma.
   Gayle et al.
   Blood, 2017;129:1768

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