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Biological Activity for Apilimod dimesylate
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.
Compound Libraries for Apilimod dimesylate
Technical Data for Apilimod dimesylate
|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.
Solubility Data for Apilimod dimesylate
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Apilimod dimesylate
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|
Product Datasheets for Apilimod dimesylate
References for Apilimod dimesylate
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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Keywords: Apilimod dimesylate, Apilimod dimesylate supplier, Phosphatidylinositol, 3-phosphate, 5-kinase, PIKfyve, inhibitors, inhibits, potent, selective, SARS-COV-2, COVID-19, B, cell, non-hodgkin, lymphoma, NHL, interleukins, IL-23, IL-12, amyotrophic, lateral, sclerosis, ALS, induces, exocytosis, Other, Kinases, Endocytosis, Cytokines, Coronavirus, Exocytosis, 7283, Tocris Bioscience
1 Citation for Apilimod dimesylate
Citations are publications that use Tocris products. Selected citations for Apilimod dimesylate include:
Markku et al (2023) SARS-CoV-2 Infection of Human Neurons Is TMPRSS2 Independent, Requires Endosomal Cell Entry, and Can Be Blocked by Inhibitors of Host Phosphoinositol-5 Kinase. J Virol 97 e0014423 PMID: 37039676
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Literature in this Area
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