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(E/Z)-BCI  ≥95%

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包装规格：10mg in glass bottle
产品描述：基本信息 产品编号： B10750 产品名称： (E/Z)-BCI CAS: 15982-84-0   储存条件 粉末 -20℃ 四年     分子式： C22H23NO 溶于液体 -80℃ 两年 分子量 317.42     化学名：  (E)-2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one Solubility (25°C)：   体外:   DMSO 63mg/mL(198.47mM) Ethanol 20mg/mL(63.0mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.1504mL 15.7520mL 31.5040mL 5mM 0.6301mL 3.1504mL 6.3008mL 10mM 0.3150mL 1.5752mL 3.1504mL 50mM 0.0630mL 0.3150mL 0.6301mL   生物活性 产品描述 一种DUSP6抑制剂，具有抗炎活性。(E/Z)-BCI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。 靶点 ROS () DUSP1 (Cell-free assay) 8.0μM(EC50) DUSP6 (Cell-free assay) 13.3μM(EC50) 体外研究 (E/Z)-BCI hydrochloride (2-10μM; 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 (0.5-4μM; 24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages. (E/Z)-BCI hydrochloride (0.5-2μM; 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. (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 the gastric cancer (GC) cells Cell Viability Assay Cell Line: Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823,mgC803, SNU216, NUGC4), AGS cell lines Concentration: 2μM,4μM,6μM,8μM,10μM Incubation Time: 72 hours Result: Cell viability was significantly decreased in a time and dose-dependent manner. Western Blot Analysis Cell Line: RAW264.7 macrophage cells (by LPS-activated macrophages) Concentration: 0.5μM,1μM,2μM,4μM Incubation Time: 24 hours Result: DUSP6 protein was significantly downregulated in LPS-activated macrophages. RT-PCR Cell Line: RAW264.7 macrophage cells (by LPS-activated macrophages) Concentration: 0.5μM,1μM,2μM Incubation Time: 24 hours Result: The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited in LPS-activated macrophages. 体内研究 (E/Z)-BCI hydrochloride (35mg/kg; intraperitoneal injection; every 7 days; for four weeks; female BALB/c nude mice) treatment enhances cisplatin efficacy in PDX models Animal Model: Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice) Dosage: 35mg/kg Administration: Intraperitoneal injection; every 7 days; for four weeks Result: Tumor weights in the PDX models treated plus CDDP were significantly suppressed compared with tumors from PDX model mice treated with either agent alone.
保存条件：-20℃

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