Chelerythrine Chloride
(Synonyms: 盐酸白屈菜红碱) 目录号 : GC13065Potent inhibitor of PKC and Bcl-xL
Cas No.:3895-92-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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). |
Animal experiment: | 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. |
References: [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. |
Chelerythrine is a potent, selective antagonist of PKC (protein kinase C) with IC50 value of 0.66 μM.[1]
The alkaloid chelerythrine is a highly specific inhibitor that acts at the regulatory domain of the kinase.[2] It is also a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP.[1] Chelerythrine induced a dose-dependent decrease in the cell viability with IC50 value of 2.6 μM measured by MTT reduction assay.[3] Chelerythrine is also a selective and strong inhibitor of Bcl-xL functions and induced cell death in MEF cells with IC50 value of 1.1 μM.[4] Chelerythrine activated MEKK1- and MKK4-dependent JNK1 and p38 pathways then mediated the induction of apoptosis.[5] Chelerythrine stimulated apoptosis in the in vivo rat experiments (5 mg/kg) by inducing the generation of reactive oxygen species.[6] Chelerythrine also has widespread physiological effects on primarily antimicrobial and anti-inflammatory.
References:
1. J. M. Herbert, J. M. Augereau, J. Gleye and J. P. Maffrand, Biochem Biophys Res Commun 1990, 172, 993-999.
2. W. D. Jarvis, A. J. Turner, L. F. Povirk, R. S. Traylor and S. Grant, Cancer Res 1994, 54, 1707-1714.
3. J. Vrba, P. Dolezel, J. Vicar, M. Modriansky and J. Ulrichova, Toxicol In Vitro 2008, 22, 1008-1017.
4. M. Vogler, K. Weber, D. Dinsdale, I. Schmitz, K. Schulze-Osthoff, M. J. Dyer and G. M. Cohen, Cell Death Differ 2009, 16, 1030-1039.
5. R. Yu, S. Mandlekar, T. H. Tan and A. N. Kong, J Biol Chem 2000, 275, 9612-9619.
6. S. Yamamoto, K. Seta, C. Morisco, S. F. Vatner and J. Sadoshima, J Mol Cell Cardiol 2001, 33, 1829-1848.
Cas No. | 3895-92-9 | SDF | |
别名 | 盐酸白屈菜红碱 | ||
化学名 | 1,2-dimethoxy-12-methyl-[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium | ||
Canonical SMILES | C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-] | ||
分子式 | C21H18ClNO4 | 分子量 | 383.83 |
溶解度 | ≥ 19.2 mg/mL in DMSO, ≥ 9.45 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6053 mL | 13.0266 mL | 26.0532 mL |
5 mM | 0.5211 mL | 2.6053 mL | 5.2106 mL |
10 mM | 0.2605 mL | 1.3027 mL | 2.6053 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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