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(E/Z)-BCI
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(E/Z)-BCI图片
CAS NO:15982-84-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
NSC 150117
产品介绍
(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].

IC50& Target

DUSP6[1]

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.
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.
分子量

317.42

Formula

C22H23NO

CAS 号

15982-84-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.