Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Chelerythrine chloride 是一种可渗透细胞的蛋白激酶 C 抑制剂,对磷酸盐受体具有竞争性,而对 ATP 是非竞争性的。它诱导细胞凋亡和自噬。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,480 | 现货 | ||
50 mg | ¥ 2,820 | 现货 | ||
100 mg | ¥ 4,220 | 现货 | ||
500 mg | ¥ 9,160 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 498 | 现货 |
产品描述 | Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP. |
靶点活性 | PKC:660 nM. |
体外活性 | Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM. It displaced Bax, a BH3-containing protein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis with characteristic features that suggest involvement of the mitochondrial pathway[1]. Chelerythrine treatment inhibits LPS-induced TNF-α level and NO production in LPS-induced murine peritoneal macrophages through selective inhibition of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) activation. In addition, the effects of chelerythrine on NO and cytokine TNF-α production can possibly be explained by the role of p38 MAPK and ERK1/2 in the regulation of inflammatory mediators expression[2]. Chelerythrine shows cytotoxic effect on the human monocytic leukaemia cells with LD50 value of 3.46 μM. Two hours after LPS stimulation, cells influenced by sanguinarine and Chelerythrine significantly decline the CCL-2 expression by a factors of 3.5 and 1.9[3]. Chelerythrine chloride significantly enhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrine chloride inhibits the phosphorylation of p38[4]. |
体内活性 | Chelerythrine shows significant anti-inflammatory effects in experimentally induced mice, endotoxic shock model, in vivo through inhibition of LPS-induced tumor necrosis factor-alpha (TNF-α) level and nitric oxide (NO) production in serum[2]. Chelerythrine chloride (5 mg/kg/day, i.p.) induces apoptosis of RCC cells without significant toxicity to mice. Chelerythrine Chloride treatment leads to the accumulation of p53 in a dose-dependent manner[4]. |
细胞实验 | Chelerythrine is dissolved in DMSO. 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). |
别名 | 白屈菜红碱, 盐酸白屈菜红碱 |
分子量 | 383.83 |
分子式 | C21H18ClNO4 |
CAS No. | 3895-92-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.8 mg/mL(10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6053 mL | 13.0266 mL | 26.0532 mL | 65.133 mL |
5 mM | 0.5211 mL | 2.6053 mL | 5.2106 mL | 13.0266 mL | |
10 mM | 0.2605 mL | 1.3027 mL | 2.6053 mL | 6.5133 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Chelerythrine chloride 3895-92-9 Apoptosis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling BCL PKC Protein kinase C 白屈菜红碱 inhibit 盐酸白屈菜红碱 Bcl-2 Family Chelerythrine Chloride Chelerythrine Inhibitor inhibitor