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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PIKfyve-AS2795440
AS2795440

Chemical Structure : AS2795440

CAS No.: 2171506-45-7

AS2795440 (AS 2795440;AS-2795440)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 480.62
分子式 C29H32N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Terajima M, et al. Eur J Pharmacol. 2016 Jun 5;780:93-105.

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