1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphatase Apoptosis
  3. (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

(E/Z)-BCI Chemical Structure

CAS No. : 15982-84-0

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Based on 1 publication(s) in Google Scholar

Other Forms of (E/Z)-BCI:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE (E/Z)-BCI

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  • Purity & Documentation

  • References

  • Customer Review

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.

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.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (315.04 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1504 mL 15.7520 mL 31.5040 mL
5 mM 0.6301 mL 3.1504 mL 6.3008 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1504 mL 15.7520 mL 31.5040 mL 78.7600 mL
5 mM 0.6301 mL 3.1504 mL 6.3008 mL 15.7520 mL
10 mM 0.3150 mL 1.5752 mL 3.1504 mL 7.8760 mL
15 mM 0.2100 mL 1.0501 mL 2.1003 mL 5.2507 mL
20 mM 0.1575 mL 0.7876 mL 1.5752 mL 3.9380 mL
25 mM 0.1260 mL 0.6301 mL 1.2602 mL 3.1504 mL
30 mM 0.1050 mL 0.5251 mL 1.0501 mL 2.6253 mL
40 mM 0.0788 mL 0.3938 mL 0.7876 mL 1.9690 mL
50 mM 0.0630 mL 0.3150 mL 0.6301 mL 1.5752 mL
60 mM 0.0525 mL 0.2625 mL 0.5251 mL 1.3127 mL
80 mM 0.0394 mL 0.1969 mL 0.3938 mL 0.9845 mL
100 mM 0.0315 mL 0.1575 mL 0.3150 mL 0.7876 mL
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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.

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Product Name:
(E/Z)-BCI
Cat. No.:
HY-126390
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