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

(E/Z)-BCI hydrochloride (Synonyms: NSC 150117 hydrochloride)

Cat. No.: HY-115502A Purity: 99.78%
Handling Instructions

(E/Z)-BCI hydrochloride (NSC 150117 hydrochloride) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI hydrochloride attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

For research use only. We do not sell to patients.

(E/Z)-BCI hydrochloride Chemical Structure

(E/Z)-BCI hydrochloride Chemical Structure

CAS No. : 95130-23-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 973 In-stock
Estimated Time of Arrival: December 31
1 mg USD 250 In-stock
Estimated Time of Arrival: December 31
5 mg   Get quote  
10 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

(E/Z)-BCI hydrochloride (NSC 150117 hydrochloride) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI hydrochloride 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].

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) 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.
Molecular Weight

353.89

Formula

C₂₂H₂₄ClNO

CAS No.

95130-23-7

SMILES

O=C1/C(C(NC2CCCCC2)C3=C1C=CC=C3)=C/C4=CC=CC=C4.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 15.62 mg/mL (44.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8257 mL 14.1287 mL 28.2574 mL
5 mM 0.5651 mL 2.8257 mL 5.6515 mL
10 mM 0.2826 mL 1.4129 mL 2.8257 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.56 mg/mL (4.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.56 mg/mL (4.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.56 mg/mL (4.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.78%

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Keywords:

(E/Z)-BCINSC 150117NSC150117NSC-150117PhosphataseDUSP6LPSROSNrf2NF-κBanti-inflammatoryERKdeathapoptosisgastric cancerInhibitorinhibitorinhibit

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(E/Z)-BCI hydrochloride
Cat. No.:
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