Apilimod

製品コードS6414 バッチS641404

印刷

化学情報

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

2 mg/mL (4.77 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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]. This compound 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.

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].

This compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/23890009/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150535/
https://pubmed.ncbi.nlm.nih.gov/17053051/

https://pubmed.ncbi.nlm.nih.gov/28104689/

+ 展开

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：

Evidence that mitochondria in macrophages are destroyed by microautophagy [ Nat Commun, 2025, 16(1):8123]	PubMed: 40885798
An advanced toolset to manipulate and monitor subcellular phosphatidylinositol 3,5-bisphosphate [ J Cell Biol, 2025, 224(6)e202408158]	PubMed: 40138452
The lipid phosphatase INPP4B controls pancreatic cancer cell migration and invasion by regulating fibronectin exocytosis [ J Biol Chem, 2025, 301(10):110716]	PubMed: 40962057
Inhibition of PIKfyve Leads to Lysosomal Disorders via Dysregulation of mTOR Signaling [ Cells, 2024, 13(11)953]	PubMed: 38891085
PIKfyve controls dendritic cell function and tumor immunity [ bioRxiv, 2024, 2024.02.28.582543]	PubMed: 38464258
PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2 [ bioRxiv, 2024, 2024.04.15.589676]	PubMed: 38659941
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

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。

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