Apilimod

製品コードS6414 バッチS641403

印刷

化学情報

Chemical Structure Synonyms STA-5326 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C23H26N6O2
分子量 418.49 CAS No. 541550-19-0
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HeLa cells
濃度 10 nM and 1 μM
反応時間 120 min
実験の流れ

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.
動物実験 動物モデル Mice
投薬量 50 mg/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。