JSH-23 是NF-Κb抑制剂，作用于脂多糖刺激的巨噬细胞 RAW 264.7，抑制 NF-Κb 转录活性(IC50=7.1 μM)，抑制 NF-Κb p65 的核易位而不影响 IκBα 降解。

JSH-23, an NF-κB inhibitor（IC50= 7.1 μM）, suppresses the transcriptional activity.

在糖尿病大鼠体内,JSH-23（3 mg/kg）能够减少神经炎症,并提高抗氧化防御明显逆转神经传导,最终改善神经血流量不足.

在RAW 264.7细胞中,JSH-23<100 μM时没有表现出明显的毒性作用,同时能够抑制脂多糖诱导的凋亡染色质浓缩。在老鼠小脑原代细胞中,JSH-23抑制脂多糖诱导的NF-κB p65核转运,而不影响IκBα降解。

Measurement of NF-κB transcriptional activity: Macrophages RAW 264.7 transfected stably with reporter plasmid of pNF-κB-SEAP-NPT are treated with 1 μg/ml LPS and/or sample for 16 hours. As the reporter, SEAP activity in the cell-free culture media is measured as followed. Single cell-derived stable transfectants are plated in 5 ml of T-25 flask, and the media is decanted 24 h later. At this time, cells are washed twice with phosphate-buffered saline, and incubations are initiated by addition of new media. Chemicals are added to the culture medium after 24 h of incubations. Aliquots (25 ml) of medium from a control or chemical-treated cultures are taken at 0, 3, 20, 24, 48, and 72 h, heated at 65°C for 5 min to eliminate the alkaline phosphatase activity, and used immediately or stored at -20°C. Mixtures consisting of dilution buffer (25 ml), assay buffer (97 ml), culture media (25 ml), and 4-methylumbelliferyl phosphate (MUP, 1 mM, 3 ml) in each well of the 96-well plates are incubated for 60 min in the dark at room temperature. Fluorescence emits the product of the SEAP/MUP is measured at 449 nm using a 96-well plate fluorometer after excitation at 360 nm.

Macrophages RAW 264.7 are incubated with various concentrations of JSH-23 compound for 24 h. The cells are treated with WST-1 solution and absorbance is measured at 450 nm.(Only for Reference)

749886-87-1

C16H20N2

240.35

JSH-23

DMSO:45 mg/mL (187.2 mM)
Ethanol:16 mg/mL (66.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years