AS2677131

AS2677131 is a potent and orally active PIKfyve inhibitor. AS2677131 inhibits f IL-12p40, IL-6 and IL-1β through a PIKfyve-c-Rel pathway. AS2677131 selectively inhibits DNA-binding activity of c-Rel to IL-12p40 and IL-1β promoter. AS2677131 inhibits MHC class II expression on B cells. AS2677131 can be used for the researches of inflammation and immunology, such as arthritis^[1]. In Vitro:AS2677131 inhibits IL-12p40 production with an IC₅₀ of 2.4 nM and inhibits IL-1β and IL-6 levels in RAW264.7 mouse macrophage cells^[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse peritoneal macrophages^[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse bone marrow-derived dendritic cells^[1].
AS2677131 (10 μM) shows no significant effect on intracellular Ca²⁺ influx in Ramos cells^[1].
AS2677131 (200 nM) inhibits PI (3,5) P₂ production by more than 90% in RAW264.7 cells^[1].
AS2677131 (100 nM, 2 h) increases the size of RAW264.7 cells and induces numerous small vesicles in the cytoplasm^[1].
AS2677131 (10-100 nM, 2h) decreases the promoter activity and inhibits the binding of c-Rel to the promoters of IL-12p40 and IL-1β in RAW264.7 cells^[1].
AS2677131 (100 nM, 2 h) reduces p-Akt levels in RAW264.7 cells^[1].
In Vivo:AS2677131 (1-30 mg/kg, p.o.) decreases the plasma levels of IL-12p40, IL-6, and TNFα in rats treated with Poly (I:C) (HY-107202) and MDP (HY-127090)^[1].
AS2677131 (1-10 mg/kg, p.o.) reduces the expression of MHC class II molecules on the surface of CD45R⁺ B cells in rats^[1].
AS2677131 (1-10 mg/kg, p.o., daily for 24 days) reduces inflammation in rats with adjuvant-induced arthritis^[1].