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

(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.

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(E/Z)-BCI Chemical Structure

(E/Z)-BCI Chemical Structure

CAS No. : 15982-84-0

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(E/Z)-BCI Related Antibodies

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Description

(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]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(E/Z)-BCI Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

317.42

Formula

C22H23NO
CAS No.
SMILES

O=C1/C(C(NC2CCCCC2)C3=C1C=CC=C3)=C\C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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(E/Z)-BCI Related Classifications

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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.

Keywords:

(E/Z)-BCI15982-84-0NSC 150117NSC150117NSC-150117PhosphataseApoptosisDUSP6LPSROSNrf2NF-κBanti-inflammatoryERKdeathapoptosisgastric cancerInhibitorinhibitorinhibit

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