(E/Z)-BCI 是一种DUSP6抑制剂,可通过激活 Nrf2 信号和抑制 NF-Κb 通路,减弱 LPS 诱导的巨噬细胞炎症和 ROS 生成,具有抗炎活性。
产品描述
(E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway. (E/Z)-BCI is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities.
体外活性
(E/Z)-BCI hydrochloride (2-10 μM;?72 hours) significantly decreases cell viability in a time and dose-dependent manner in gastric epithelial cell GES1, GC cell lines, and AGS cell lines.?(E/Z)-BCI hydrochloride (0.5-4 μM;?24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages. (E/Z)-BCI hydrochloride inhibits cell proliferation, migration, and invasion in a receptor-independent manner and enhances Cisplatin (CDDP) cytotoxicity (enhances CDDP-induced cell death and apoptosis) at pharmacological concentrations in gastric cancer (GC) cells.?(E/Z)-BCI hydrochloride (0.5-2 μM;?24 hours) treatment significantly inhibits the expression of IL-1β, TNF-α, and IL-6 mRNA in LPS-activated macrophages.?(E/Z)-BCI hydrochloride decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages.?
体内活性
(E/Z)-BCI hydrochloride treatment enhances cisplatin efficacy in PDX models.
Cas No.
15982-84-0
分子式
C22H23NO
分子量
317.42
别名
NSC 150117
储存和溶解度
Ethanol:20mg/mL (60.00mM),Need ultrasonic
DMSO:60mg/mL (189.02mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years