Apilimod dimesylate

Product Description

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.

Solubility

Preparing Stock Solutions for Apilimod dimesylate

The following data is based on the product molecular weight 610.70

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product.

• Hung PIKFYVE inhibition mitigates disease in models of diverse forms of ALS. Cell 2023 PMID: 36754049
• Gayle Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 2017 PMID: 28104689
• Ou Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 2020 PMID: 32221306
• Riva Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature 2020 PMID: 32707573
• Cai 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. 2013 PMID: 23890009
• Wada Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 2007 PMID: 17053051