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Dual Specificity Protein Phosphatase 1/6 Inhibitor
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- CAS号:
- 15982-84-0
- 英文名:
- Dual Specificity Protein Phosphatase 1/6 Inhibitor
- 英文别名:
- NSC 150117;(E/Z)-BCI (NSC150117);(E/Z)-BCI(DUSP6 inhibitor);Dual Specificity Protein Phosphatase 1/6 Inhibitor;2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one;1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-;NSC-150117,ROS,death,LPS,(E/Z)-BCI,gastric cancer,anti-inflammatory,NF-κB,inhibit,Inhibitor,(E/Z) BCI,Nrf2,(E/Z)BCI,Apoptosis,ERK,Phosphatase,DUSP6,NSC150117
- 中文名:
- Dual Specificity Protein Phosphatase 1/6 Inhibitor
- 中文别名:
- 化合物(E/Z)-BCI;2-亚苄基-3-(环己基氨基)-2,3-二氢-1H-茚-1-酮
- CBNumber:
- CB35544728
- 分子式:
- C22H23NO
- 分子量:
- 317.42
- MOL File:
- 15982-84-0.mol
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Dual Specificity Protein Phosphatase 1/6 Inhibitor化学性质
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沸点:
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484.6±45.0 °C(Predicted)
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密度:
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1.15±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C(protect from light)
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溶解度:
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DMSO: 63 mg/mL (198.48 mM);Ethanol: 20 mg/mL (63.01 mM)
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酸度系数(pKa):
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7.74±0.20(Predicted)
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水溶解性:
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Water: Insoluble
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Dual Specificity Protein Phosphatase 1/6 Inhibitor性质、用途与生产工艺
(E/Z)-BCI (BCI, NSC 150117) 是一种 dual specific phosphatase 1/6 (DUSP1/DUSP6) 和 mitogen-activated protein kinase 的抑制剂，对细胞中DUSP6和DUSP1的EC50值分别为13.3 μM和8.0 μM。(E)-BCI 在H1299肺癌细胞中通过产生 reactive oxygen species (ROS) 和激活内在的线粒体途径来诱导凋亡。
| Target | Value |
ROS
()
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DUSP1
(Cell-free assay)
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8.0 μM(EC50)
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DUSP6
(Cell-free assay)
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13.3 μM(EC50)
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(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.
(E/Z)-BCI hydrochloride (0.5-4 μM; 24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages.
(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.
(E/Z)-BCI hydrochloride decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages.
(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.
Cell Viability Assay
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Cell Line:
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Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines
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Concentration:
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2 μM, 4 μM, 6 μM, 8 μM, 10 μM
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Incubation Time:
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72 hours
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Result:
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Cell viability was significantly decreased in a time and dose-dependent manner.
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Western Blot Analysis
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Cell Line:
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RAW264.7 macrophage cells (by LPS-activated macrophages)
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Concentration:
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0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:
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24 hours
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Result:
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DUSP6 protein was significantly downregulated in LPS-activated macrophages.
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RT-PCR
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Cell Line:
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RAW264.7 macrophage cells (by LPS-activated macrophages)
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Concentration:
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0.5 μM, 1 μM, 2 μM
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Incubation Time:
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24 hours
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Result:
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The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited in
LPS-activated macrophages.
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(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.
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Animal Model:
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Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice)
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Dosage:
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35 mg/kg
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Administration:
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Intraperitoneal injection; every 7 days; for four weeks
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Result:
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Tumor weights in the PDX models treated plus CDDP were significantly suppressed compared with tumors from PDX model mice treated with either agent alone.
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Dual Specificity Protein Phosphatase 1/6 Inhibitor
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | S0056 | (E/Z)-BCI | 15982-84-0 | 10mM (1mL in DMSO) | 2432.43元 |
| 2024/04/30 | S0056 | Dual Specificity Protein Phosphatase 1/6 Inhibitor
(E/Z)-BCI | 15982-84-0 | 25mg | 8790.18元 |
Dual Specificity Protein Phosphatase 1/6 Inhibitor
生产厂家
15982-84-0, Dual Specificity Protein Phosphatase 1/6 Inhibitor 相关搜索:
- 药靶配体
- 化合物(E/Z)-BCI
- 2-亚苄基-3-(环己基氨基)-2,3-二氢-1H-茚-1-酮
- 15982-84-0
- NSC-150117,ROS,death,LPS,(E/Z)-BCI,gastric cancer,anti-inflammatory,NF-κB,inhibit,Inhibitor,(E/Z) BCI,Nrf2,(E/Z)BCI,Apoptosis,ERK,Phosphatase,DUSP6,NSC150117
- 2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one
- (E/Z)-BCI(DUSP6 inhibitor)
- 1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-
- (E/Z)-BCI (NSC150117)
- NSC 150117
- Dual Specificity Protein Phosphatase 1/6 Inhibitor