Apilimod

For research use only.

Catalog No.S6414 Synonyms: STA-5326

1 publication

Apilimod Chemical Structure

Molecular Weight(MW): 418.49

Apilimod (STA-5326) is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.

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Selleck's Apilimod has been cited by 1 publication

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Choose Selective PIKfyve Inhibitors

Biological Activity

Description Apilimod (STA-5326) is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Targets
PIKfyve [1]
()
14 nM
In vitro

Apilimod selectively inhibits TLR-induced cytokine expression. It selectively inhibits the production of IL12p40, whereas it has little effect on IL8 production in THP-1 cells[1]. Apilimod reduces not only PtdIns(3,5)P2 production but also that of PtdIns5P in intact cells[2].

Protocol

Cell Research:

[1]

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  • Cell lines: HeLa cells
  • Concentrations: 10 nM and 1 μM
  • Incubation Time: 120 min
  • Method:

    HeLa cells are metabolically labeled with [3H]inositol for 72 hr and treated with two doses of apilimod or the inactive analog API09 for 120 min. Lipids are extracted, deacetylated, and analyzed by HPLC.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (200.72 mM)
Ethanol '''-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 418.49
Formula

C23H26N6O2

CAS No. 541550-19-0
Storage powder
in solvent
Synonyms STA-5326
Smiles CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00234741 Completed Drug: STA-5326 mesylate Crohn''s Disease Synta Pharmaceuticals Corp.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) November 2005 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID