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Apilimod

Chemical Structure : Apilimod

CAS No.: 541550-19-0

Apilimod (STA-5326;STA 5326)

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

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).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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); suppresses Th1 but not Th2 immune response in mice; binds to PIKfyve and blocks its phosphotransferase activity (IC50=14 nM), has no activity on PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms; also potently blocks infections by EBOV and MARV in Huh 7, Vero E6 and primary human macrophage cells with IC50 of 10 nM.

Blood Cancer

Phase 2 Clinical

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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