上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
(E/Z)-BCI (Synonyms: NSC 150117)
(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。
(E/Z)-BCI Chemical Structure
CAS No. : 15982-84-0
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (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 the NF-κB pathway[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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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| 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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| 参考文献 |
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[1]. Zhang F, et al. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681.
[2]. Wu QN,et al. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255.
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