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Apilimod

Chemical Structure : Apilimod

CAS No.: 541550-19-0

Apilimod (STA-5326, STA5326)

Catalog No.: PC-60412Not For Human Use, Lab Use Only.

Apilimod (STA5326) is a potent IL-12/IL-23 inhibitor that down-regulates both IL-12 p35 and IL-12/IL-23 p40 at the transcriptional level, and inhibits the production of both IL-12 and IL-23 cytokines (IC50=2 nM), inhibits PIKfyve phosphotransferase activity (IC50=14 nM).

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Biological Activity

Apilimod (STA5326) is a potent IL-12/IL-23 inhibitor that down-regulates both IL-12 p35 and IL-12/IL-23 p40 at the transcriptional level, and inhibits the production of both IL-12 and IL-23 cytokines (IC50=2 nM), inhibits PIKfyve phosphotransferase activity (IC50=14 nM).
Apilimod (STA5326) suppresses Th1 but not Th2 immune response in mice.
Apilimod (STA5326) binds to PIKfyve and blocks its phosphotransferase activity (IC50=14 nM), has no activity on PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms.
Apilimod (STA5326) also potently blocks infections by EBOV and MARV in Huh 7, Vero E6 and primary human macrophage cells with IC50 of 10 nM.

Physicochemical Properties

M.Wt 418.49
Formula C23H26N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzaldehyde, 3-methyl-, [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone (9CI)

References

1. Wada Y, et al. Blood. 2007 Feb 1;109(3):1156-64.

2. Cai X, et al. Chem Biol. 2013 Jul 25;20(7):912-21.

3. Nelson EA, et al. PLoS Negl Trop Dis. 2017 Apr 12;11(4):e0005540.

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