Apilimod
Apilimod (STA 5326) is a selective inhibitor of the PIKfyve kinase. It acts on the PIKfyve pathway to regulate intracellular phospholipid metabolism, thereby affecting multiple cellular biological processes. In addition, it inhibits the production of cytokines IL-12/IL-23 mediated by human- or monkey-derived PBMCs (IC50 of 1 nM and 2 nM, respectively). Based on the above mechanism of action, Apilimod is commonly used to study signaling pathways related to inflammation, autoimmune responses, vesicular transport, and lysosomal function.
| Physical Appearance | A solid |
| Storage | -20°C |
| M.Wt | 418.49 |
| Cas No. | 541550-19-0 |
| Formula | C23H26N6O2 |
| Synonyms | STA-5326 |
| Solubility | insoluble in H2O; ≥17.9 mg/mL in DMSO; ≥6.86 mg/mL in EtOH with ultrasonic |
| Chemical Name | (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine |
| Canonical SMILES | CC1=CC(/C([H])=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=CC=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Human and monkey PBMCs |
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Preparation method |
The solubility of this compound in DMSO is >17.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
8 to 1000 nM |
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Applications |
Apilimod inhibited IFN-r production induced by either IFN-/SAC or SAC in human PBMCs. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J miceimmunised with human interphotoreceptor retinoid binding protein peptide (IRBP1–20) |
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Dosage form |
5 mg/kg or 20 mg/kg; orally administered; once a day for six days a week from day 0 to day 14. |
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Application |
Oral administration of either 5 mg/kg or 20 mg/kg apilimod reduced the severity of EAU (experimental autoimmune uveoretinitis) on day 14 and 18. In addition, mice treated with 20 mg/kg apilimod showed significantly decreased severity of EAU by histopathological analysis. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] . Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122. [2].Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64. |
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Quality Control & MSDS
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Chemical structure
