Dual Specificity Protein Phosphatase 1/6 Inhibitor
| 中文名称 | Dual Specificity Protein Phosphatase 1/6 Inhibitor |
|---|---|
| 中文同义词 | 2-亚苄基-3-(环己基氨基)-2,3-二氢-1H-茚-1-酮;化合物(E/Z)-BCI |
| 英文名称 | Dual Specificity Protein Phosphatase 1/6 Inhibitor |
| 英文同义词 | Dual Specificity Protein Phosphatase 1/6 Inhibitor;NSC 150117;(E/Z)-BCI (NSC150117);1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-;(E/Z)-BCI(DUSP6 inhibitor);2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one;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 |
| CAS号 | 15982-84-0 |
| 分子式 | C22H23NO |
| 分子量 | 317.42 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 15982-84-0.mol |
| 结构式 |  |
Dual Specificity Protein Phosphatase 1/6 Inhibitor 性质
| 沸点 | 484.6±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.15±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | DMSO：63 mg/mL (198.48 mM)；乙醇：20 mg/mL (63.01 mM) |
| 酸度系数(pKa) | 7.74±0.20(Predicted) |
| 水溶解性 | Water: Insoluble |
| Target | Value |
|
ROS
() | |
|
DUSP1
(Cell-free assay) | 8.0 μM(EC50) |
|
DUSP6
(Cell-free assay) | 13.3 μM(EC50) |
(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
| 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
| 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
| 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. |
(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.
| Animal Model: | Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice) |
| 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. |
安全信息
| 海关编码 | 2922390090 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS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 |