Apilimod

Catalog No.S6414 Batch:S641402

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Technical Data

Formula

C23H26N6O2
Molecular Weight 418.49 CAS No. 541550-19-0
Solubility (25°C)* In vitro DMSO 84 mg/mL (200.72 mM)
Ethanol 6 mg/mL (14.33 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Apilimod 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
IL-12 [1]
( in IFN-γ/SAC-stimulated human PBMCs)		 IL-12 [1]
(in human monocytes)		 IL-12 [1]
(in mouse PBMCs)		 PIKfyve [1]
1 nM 1 nM 2 nM 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].
In vivo

Apilimod is a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma.

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[4]
  • Animal Models

    Mice

  • Dosages

    50 mg/kg

  • Administration

    p.o.

Selleck's Apilimod has been cited by 14 publications

PIKfyve controls dendritic cell function and tumor immunity [ bioRxiv, 2024, 2024.02.28.582543] PubMed: 38464258
Simultaneous inhibition of endocytic recycling and lysosomal fusion sensitizes cells and tissues to oligonucleotide therapeutics [ Nucleic Acids Res, 2023, 51(4):1583-1599] PubMed: 36727438
Apilimod activates the NLRP3 inflammasome through lysosome-mediated mitochondrial damage [ Front Immunol, 2023, 14:1128700] PubMed: 37359517
Executable network of SARS-CoV-2-host interaction predicts drug combination treatments [ NPJ Digit Med, 2022, 5(1):18] PubMed: 35165389
Executable network of SARS-CoV-2-host interaction predicts drug combination treatments [ NPJ Digit Med, 2022, 5(1):18] PubMed: 35165389
Selective elimination of pluripotent stem cells by PIKfyve specific inhibitors [ Stem Cell Reports, 2022, 17(2):397-412] PubMed: 35063131
PIKfyve-specific inhibitors restrict replication of multiple coronaviruses in vitro but not in a murine model of COVID-19 [ Commun Biol, 2022, 5(1):808] PubMed: 35962188
TSC1 binding to lysosomal PIPs is required for TSC complex translocation and mTORC1 regulation [ Mol Cell, 2021, S1097-2765(21)00324-5] PubMed: 33974911
SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation [ Elife, 2021, 10e65962] PubMed: 33890572
Mitochondria-lysosome membrane contacts are defective in GDAP1-related Charcot-Marie-Tooth disease [ Hum Mol Genet, 2021, 29(22):3589-3605] PubMed: 33372681

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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