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Apilimod
- STA 5326- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H26N6O2
- MW: 418.49
Description
Apilimod is a potent and selective PIKfyve lipid kinase inhibitor that reduces synthesis of phosphatidylinositol 3,5-bisphosphate and disrupts endolysosomal membrane trafficking.
PIKfyve controls endosome maturation, lysosomal homeostasis and autophagic flux. Apilimod therefore produces characteristic endolysosomal vacuolation and is widely used to investigate PIKfyve-dependent trafficking, pathogen entry and cancer-cell vulnerabilities; its earlier description as an IL-12/IL-23 inhibitor reflects downstream immunological effects.
Key Features
- Potent and selective PIKfyve lipid kinase inhibitor
- Disrupts endosome-to-lysosome trafficking and lysosomal homeostasis
- Induces endolysosomal vacuolation through phosphoinositide depletion
- Useful for linking PIKfyve activity to autophagy and immune signaling
Applications
- PIKfyve and phosphoinositide signaling studies
- Endolysosomal trafficking and lysosome biology
- Autophagy and vacuolation assays
- Pathogen-entry and PIKfyve-dependent cancer models
The water-soluble dimesylate salt form, Apilimod dimesylate (Axon 2500), is available as well.
Note: Apilimod (Axon 1369) or Apilimod dimesylate (Axon 2500) from Axon Medchem are fully QC-ed drug reference standards with approved bioactivities. Several prominent research laboratories have tested our samples with satisfactory testing results, evidenced by recent publications. There used to be the wrong isomer of Apilimod and its mesylate salt appeared on the reagent market from some other sources, which would be inactive in your assays. Be right about your drug!
More Information
| Parent CAS No. | 541550-19-0 |
|---|---|
| Chemical Name | N-[6-Morpholin-4-yl-2-(2-pyridin-2-yl-ethoxy)-pyrimidin-4-yl]-N'-[1-m-tolyl-meth-(E)-ylidene]-hydrazine |
| SMILES | C1(OCCC2N=CC=CC=2)N=C(N/N=C/C2C=CC=C(C)C=2)C=C(N2CCOCC2)N=1 |
| MFCD | MFCD09954108 |
| InChi | InChI=1S/C23H26N6O2/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28)/b25-17+ |
| InChiKey | HSKAZIJJKRAJAV-KOEQRZSOSA-N |
| CID | 10173277 |
| Short Description | IL-12/23 and PIKfyve inhibitor |
References
- Wada et al: Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood, 2007, 109(3), 1156-1164.
- Wada et al: IL-12/IL-23 inhibitors: a promising approach to the treatment of inflammatory disorders. Drugs Fut. 2008, 33(1), 49-63.
- Gayle et al: Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood, 2017, 129(13), 1768–1778
- List of publications using Apilimod (Axon 1369) and Apilimod (Axon 2500) purchased from Axon Medchem
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