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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.
Apilimod dimesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 610.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.64 mL||8.19 mL||16.37 mL|
|5 mM||0.33 mL||1.64 mL||3.27 mL|
|10 mM||0.16 mL||0.82 mL||1.64 mL|
|50 mM||0.03 mL||0.16 mL||0.33 mL|
References are publications that support the biological activity of the product.
Wada et al (2007) Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 109 1156 PMID: 17053051
Cai et al (2013) 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. Chem.Biol. 20 912 PMID: 23890009
Riva et al (2020) Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature 586 113 PMID: 32707573
Ou et al (2020) Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 11 1620 PMID: 32221306
Gayle et al (2017) Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 129 1768 PMID: 28104689
Hung et al (2023) PIKFYVE inhibition mitigates disease in models of diverse forms of ALS. Cell PMID: 36754049
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