1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphatase Apoptosis
  3. (E/Z)-BCI

(E/Z)-BCI  (Synonyms: NSC 150117)

目录号: HY-126390
产品使用指南

(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。

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(E/Z)-BCI Chemical Structure

(E/Z)-BCI Chemical Structure

CAS No. : 15982-84-0

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1 mg ¥2033
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

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].

MCE 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.
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].

MCE 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.
分子量

317.42

Formula

C22H23NO

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(E/Z)-BCI
目录号:
HY-126390
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