(E/Z)-BCI
Based on 1 publication(s) in Google Scholar
(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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- 純度: 99.38%
- CAS 番号: 15982-84-0
- 分子式: C22H23NO
- 分子量:317.42
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 (E/Z)-BCI
More
生物活性
製品説明
IC50 & Target
DUSP6[1]
体外実験
(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.
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Cell Line:Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines
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Concentration:2 μM, 4 μM, 6 μM, 8 μM, 10 μM
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Incubation Time:72 hours
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Result:Cell viability was significantly decreased in a time and dose-dependent manner.
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Cell Line:RAW264.7 macrophage cells (by LPS-activated macrophages)
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Concentration:0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 hours
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Result:DUSP6 protein was significantly downregulated in LPS-activated macrophages.
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Cell Line:RAW264.7 macrophage cells (by LPS-activated macrophages)
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 hours
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Result:The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited in LPS-activated macrophages.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice)[2]
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Dosage:35 mg/kg
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Administration:Intraperitoneal injection; every 7 days; for four weeks
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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.
化学情報
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CAS 番号 15982-84-0
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性状 Solid
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分子量 317.42
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分子式 C22H23NO
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Color Off-white to light yellow
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SMILES
O=C1/C(C(NC2CCCCC2)C3=C1C=CC=C3)=C\C4=CC=CC=C4
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別名
NSC 150117
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
DUSP6 expression is associated with osteoporosis through the regulation of osteoclast differentiation via ERK2/Smad2 signaling. [Abstract]2021 Sep 2;12(9):825. PMID: 34475393
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zhang F, et al. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681. [Content Brief]
[2]. Wu QN,et al. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255. [Content Brief]
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 |
(E/Z)-BCI 関連分類
HY-126390 関連分類
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