15982-84-0
15982-84-0 結(jié)構(gòu)式
基本信息
2-亞芐基-3-(環(huán)己基氨基)-2,3-二氫-1H-茚-1-酮
(E/Z)-BCI (NSC150117)
(E/Z)-BCI(DUSP6 inhibitor)
Dual Specificity Protein Phosphatase 1/6 Inhibitor
1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-
物理化學(xué)性質(zhì)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/11/08 | S0056 | (E/Z)-BCI | 15982-84-0 | 10mM (1mL in DMSO) | 2432.43元 |
| 2024/11/08 | S0056 | Dual Specificity Protein Phosphatase 1/6 Inhibitor (E/Z)-BCI | 15982-84-0 | 5mg | 2750.96元 |
| 2024/11/08 | S0056 | Dual Specificity Protein Phosphatase 1/6 Inhibitor (E/Z)-BCI | 15982-84-0 | 25mg | 8790.18元 |
常見問題列表
| 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. |