15982-84-0

中文名称 Dual Specificity Protein Phosphatase 1/6 Inhibitor

英文名称 Dual Specificity Protein Phosphatase 1/6 Inhibitor

CAS 15982-84-0

分子式 C22H23NO

分子量 317.42

MOL 文件 15982-84-0.mol

更新日期 2024/06/12 17:31:28

15982-84-0 结构式

基本信息物理化学性质安全数据 Dual Specificity Protein Phosphatase 1/6 Inhibitor价格(试剂级) 常见问题列表

基本信息

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

英文别名

NSC 150117
(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)-

物理化学性质

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)

储存条件Keep in dark place,Sealed in dry,2-8°C

溶解度DMSO: 63 mg/mL (198.48 mM);Ethanol: 20 mg/mL (63.01 mM)

酸度系数(pKa)7.74±0.20(Predicted)

形态solid

颜色yellow

水溶解性水：不溶

安全数据

危险性符号(GHS) GHS hazard pictograms

GHS07

警示词警告

危险性描述H302-H315-H319-H412

防范说明P273-P305+P351+P338

海关编码2922390090

Dual Specificity Protein Phosphatase 1/6 Inhibitor价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2025/09/19	S0056	(E/Z)-BCI	15982-84-0	10mM (1mL in DMSO)	2432.43元
2025/09/19	S0056	Dual Specificity Protein Phosphatase 1/6 Inhibitor (E/Z)-BCI	15982-84-0	5mg	2750.96元
2025/09/19	S0056	Dual Specificity Protein Phosphatase 1/6 Inhibitor (E/Z)-BCI	15982-84-0	25mg	8790.18元

常见问题列表

生物活性

(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。

靶点

Target	Value
ROS ()
DUSP1 (Cell-free assay)	8.0 μM(EC50)
DUSP6 (Cell-free assay)	13.3 μM(EC50)

体外研究

(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.

体内研究

(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.