| CAS |
No.3895-92-9 |
| 中文名称 |
盐酸白屈菜红碱(10mM in DMSO，无菌） |
| 英文名称 |
Chelerythrine Chloride(10mM in DMSO，Sterile) |
| 分子式 |
C21H18ClNO4 |
| 分子量 |
383.82 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 运输条件 |
冷冻运输 |
| 靶点 |
PKC |
| 通路 |
TGF-beta/Smad;Epigenetics |
| 背景说明 |
Chelerythrine Chloride 是一种 PKC抑制剂。 |
| 生物活性 |
Chelerythrine chloride is a potent， cell-permeable inhibitor of protein kinase C， with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.[1-6] |
| In Vitro |
Chelerythrine 抑制 BclXL-Bak BH3 肽结合，IC50 为 1.5 μM，并从 BclXL 中置换 Bax (一种含有 BH3 的蛋白质)。用 Chelerythrine 处理的哺乳动物细胞发生细胞凋亡，其特征表明线粒体通路参与[1]。Chelerythrine 处理通过选择性抑制 p38 丝裂原活化蛋白激酶 (MAPK) 和细胞外信号调节蛋白激酶 1 和 2 (ERK1/2) 激活，抑制 LPS 诱导的 TNF-α 水平和 LPS 诱导的小鼠腹腔巨噬细胞中的 NO 产生。此外，Chelerythrine 对 NO 和细胞因子 TNF-α 产生的影响可能可以通过 p38 MAPK 和 ERK1/2 在炎症介质表达调节中的作用来解释[2]。Chelerythrine 对人单核细胞白血病细胞具有细胞毒作用，LD50 值为 3.46 μM。LPS 刺激两小时后，受血根碱和 Chelerythrine 影响的细胞显著降低 CCL-2 表达 3.5 倍和 1.9 倍[3]。Chelerythrine chloride 以剂量依赖的方式显著增强 ERK1/2 的磷酸化。此外，chelerythrine chloride 可抑制 p38 的磷酸化[4]。 |
| In Vivo |
Chelerythrine 通过抑制 LPS 诱导的肿瘤坏死因子-α (TNF-α) 水平和血清中一氧化氮 (NO) 的产生，在体内实验诱导的小鼠内毒素休克模型中表现出显著的抗炎作用[2]。Chelerythrine chloride (5 mg/kg/day，腹腔注射) 诱导 RCC 细胞凋亡，对小鼠无显著毒性。Chelerythrine Chloride 处理会导致 p53的剂量依赖性积累[4]。 |
| 细胞实验 |
Cell viability is evaluated via MTT assay. Cells (2×103?HEK-293 cells/well and 3×103?SW-839 cells/well) in 100 μL medium are seeded into 96-well plates， and incubated for 12 h. Next， the medium in each well is replaced with medium containing various concentrations of Chelerythrine Chloride， and the cells are incubated at 37°C for an additional 24 and 48 h. Subsequently， 20 μL MTT (5 mg/mL) is added to each well. Following an additional incubation at 37°C for 4 h， the supernatant is removed， and 100 μL DMSO is added to each well. The absorbance values (read at 540 nm) are determined using the iMark? Microplate Absorbance Reader. The data are analyzed using Microplate Manager software (ver. 6.3; 1689520). |
| 动物实验 |
A total of 5×106 SW-839 cells are mixed with Matrigel?， and injected subcutaneously into the flanks of 14 5-week-old male BALB/c nude mice. The mice are maintained in 18×30-cm cages containing three mice each， at a temperature of 22°C using a 12 h light/dark cycle. Food and water is available ad libitum. The mice are randomLy divided into two groups (n=7). As previously described， the mice are administrated with chelerythrine chloride at a dose of 5 mg/kg/day via intraperitoneal injection for 5 weeks， with the first injection of chelerythrine chlorideurring 24 h after injection with the SW-839 cells. The control mice are administered with the same volume of PBS containing 1% DMSO. The volume and weight of the mouse tumors are measured once a week. All the mice are sacrificed 36 days subsequent to inoculation of the cancer cells， when the tumors are resected. |
| 数据来源文献 |
[1]. Li W， et al. Effect of Chelerythrine Against Endotoxic Shock in Mice and Its Modulation of Inflammatory Mediators in Peritoneal Macrophages Through the Modulation of Mitogen-Activated Protein Kinase (MAPK) Pathway. Inflammation. 2012 Jul 24.
[2]. Pencikova K， et al. Investigation of sanguinarine and chelerythrine effects on LPS-induced inflammatory gene expression in THP-1 cell line. Phytomedicine. 2012 Jul 15;19(10):890-5. Epub 2012 May 14.
[3]. Chen XM， et al. Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines. Oncol Lett. 2016 Jun;11(6):3917-3924
[4]. Herbert JM， et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1990 Nov 15;172(3):993-9.
[5]. Chan SL， et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6.
[6]. Tang ZH， et al.Induction of reactive oxygen species-stimulated distinctive autophagy by chelerythrine in non-small cell lung cancer cells.Redox Biol. 2017 Aug;12:367-376. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号