Chemical Structure : AS2795440
CAS No.:
2171506-45-7
AS2795440
(AS 2795440;AS-2795440)
Catalog No.: PC-60992Not For Human Use, Lab Use Only.
AS2795440 is a potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AS2795440 is a potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM).
AS2795440 inhibits the production of IL-12p40, IL-6 and IL-1β but not TNFα in activated macrophages or dendritic cells, and expression of IgM-induced MHC class II on B cells.
AS2795440 reduces Akt phosphorylation in IFNγ/LPS-stimulated RAW264.7 cells.
AS2795440 greatly increases cell size with many small vesicles in the cytoplasm; prevents the development of arthritis in rats.
Physicochemical Properties
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M.Wt
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480.62
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Formula
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C29H32N6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(1''-isopropyl-6-methyl-1'',2'',3'',6''-tetrahydro-[3,3':6',4''-terpyridin]-5-yl)-2,3-dimethyl-1H-pyrrolo[3,2-b]pyridine-5-carboxamide
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References
1. Terajima M, et al. Eur J Pharmacol. 2016 Jun 5;780:93-105.
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