(E/Z)-BCI (NSC 150117) 是一种
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。
| 生物活性 |
(E/Z)-BCI (NSC 150117) is adual-specificityphosphatase6 (DUSP6)inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting theNF-κBpathway[1].
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| IC50& Target |
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体外研究
(In Vitro) |
(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[2].
(E/Z)-BCI hydrochloride (0.5-4 μM; 24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages[1].
(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[1].
(E/Z)-BCI hydrochloride decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages[1]. (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[2].
Cell Viability Assay[2]
| Cell Line: |
Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines |
| Concentration: |
2 μM, 4 μM, 6 μM, 8 μM, 10 μM |
| Incubation Time: |
72 hours |
| Result: |
Cell viability was significantly decreased in a time and dose-dependent manner. |
Western Blot Analysis[1]
| Cell Line: |
RAW264.7 macrophage cells (by LPS-activated macrophages) |
| Concentration: |
0.5 μM, 1 μM, 2 μM, 4 μM |
| Incubation Time: |
24 hours |
| Result: |
DUSP6 protein was significantly downregulated in LPS-activated macrophages. |
RT-PCR[1]
| Cell Line: |
RAW264.7 macrophage cells (by LPS-activated macrophages) |
| Concentration: |
0.5 μM, 1 μM, 2 μM |
| Incubation Time: |
24 hours |
| Result: |
The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited in LPS-activated macrophages. |
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体内研究
(In Vivo) |
(E/Z)-BCI hydrochloride (35 mg/kg; intraperitoneal injection; every 7 days; for four weeks; female BALB/c nude mice) treatment enhances cisplatin efficacy in PDX models[2].
| Animal Model: |
Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice)[2] |
| Dosage: |
35 mg/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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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