Dual Specificity Protein Phosphatase 1/6 Inhibitor
- CAS号:15982-84-0
- 英文名:Dual Specificity Protein Phosphatase 1/6 Inhibitor
- 中文名:Dual Specificity Protein Phosphatase 1/6 Inhibitor
- CBNumber:CB35544728
- 分子式:C22H23NO
- 分子量:317.42
- MOL File:15982-84-0.mol
- 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);Ethanol: 20 mg/mL (63.01 mM)
- 酸度系数(pKa) :7.74±0.20(Predicted)
- 水溶解性 :Water: Insoluble
- 海关编码 :2922390090
Dual Specificity Protein Phosphatase 1/6 Inhibitor性质、用途与生产工艺
- 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.
- 更新日期：2024/04/30
- 产品编号：S0056
- 产品名称：(E/Z)-BCI
- CAS编号：15982-84-0
- 包装：10mM (1mL in DMSO)
- 价格：2432.43元
- 更新日期：2024/04/30
- 产品编号：S0056
- 产品名称：Dual Specificity Protein Phosphatase 1/6 Inhibitor (E/Z)-BCI
- CAS编号：15982-84-0
- 包装：25mg
- 价格：8790.18元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：19892
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57511
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
