Sanguinarine chloride
(Synonyms: 氯化血根碱; Sanguinarin chloride; Sanguinarium chloride; Pseudochelerythrine chloride) 目录号 : GC13442
A natural alkaloid with anti-inflammatory and anti-oxidant properties
Cas No.:5578-73-4
Sample solution is provided at 25 µL, 10mM.
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Sanguinarine chloride is a potent and specific inhibitor of PP2C with Ki value of 0.68 μM, and is also a selective and cell-active inhibitor of MKP-1 with IC50 value of 10 μM. Sanguinarine is also an allosteric activator of AMPK [1][2][3].
Protein phosphatase 2C (PP2C) is a serine/threonine-specific phosphatase, the activity of which is dependent on Mg2+ or Mn2+. PP2C dephosphorylates a number of substrates such as cyclin-dependent kinase, mitogen-activated kinase (MAPK) and Bad. Mitogen-activated protein kinase phosphatase-1 (MKP-1) is a dual specificity phosphatase. AMP-activated protein kinase (AMPK) plays an important role in the regulation of cellular metabolism [1][2][3].
Sanguinarine chloride is an inhibitor of PP2C and MKP-1, and also an allosteric activator of AMPK with antibiotic and antitumor activity. Sanguinarine competed with α-casein to inhibit PP2C and exhibited selectivity for PP2C as compared with PP1, PP2A and PP2B. In human promyelocytic leukemia cell line HL60, sanguinarine exhibited cytotoxicity with IC50 value of 0.37 μM and induced apoptosis via a caspase-3/7-dependent mechanism involving the phosphorylation of p38, a PP2C substrate [1]. Sanguinarine inhibited MKP-1 and MKP-L with IC50 values of 17.3 and 12.5 μM. In PANC-1 human pancreatic cancer cells, sanguinarine increased ERK and JNK/SAPK phosphorylation [2]. In the MDA MB-231 cell line, sanguinarine caused AMPK and the downstream acetyl-CoA carboxylase (ACC) phosphorylation [3]. In LNCaP and DU145 cells, sanguinarine inhibited cell growth, induced G0/G1 phase arrest and apoptosis [4].
References:
[1]. Aburai N, Yoshida M, Ohnishi M, et al. Sanguinarine as a potent and specific inhibitor of protein phosphatase 2C in vitro and induces apoptosis via phosphorylation of p38 in HL60 cells. Biosci Biotechnol Biochem, 2010, 74(3): 548-552.
[2]. Vogt A, Tamewitz A, Skoko J, et al. The benzo[c]phenanthridine alkaloid, sanguinarine, is a selective, cell-active inhibitor of mitogen-activated protein kinase phosphatase-1. J Biol Chem, 2005, 280(19): 19078-19086.
[3]. Choi J, He N, Sung MK, et al. Sanguinarine is an allosteric activator of AMP-activated protein kinase. Biochem Biophys Res Commun, 2011, 413(2): 259-263.
[4]. Adhami VM, Aziz MH, Reagan-Shaw SR, et al. Sanguinarine causes cell cycle blockade and apoptosis of human prostate carcinoma cells via modulation of cyclin kinase inhibitor-cyclin-cyclin-dependent kinase machinery. Mol Cancer Ther, 2004, 3(8): 933-940.
Kinase experiment: | The caspase-3 activity is measured using a caspase-3 activity assay kit. Briefly, the cells treated by different concentrations of Sanguinarine (0.5 μM, 1 μM, 2 μM, 4 μM) or control DMSO are collected, washed and lysed in a lysis buffer for 30 min on ice. The supernatants are then collected by centrifuging at 1,2000 rpm for 10 min. The Ac-DEVD-pNA (2 mM) is added to each sample and incubated at 37°C for 1 h. The optical density (OD) of each sample is finally quantified at a wavelength of 405 nm using a spectrophotometer. The p-NA standard is used to calibrate the caspase-3 activity of each sample[1]. |
Cell experiment: | The cell viability of Sanguinarine is determined by CCK-8 assay using a cell counting kit-8. Briefly, 22B-cFluc cells are seeded in a 96-well plate (5×103 cells/well) and treated with different concentrations of Sanguinarine (0.5 μM, 1 μM, 2 μM, 4 μM) for 24 h. Then 10 mL CKK-8 is added to each well for 4 h and the absorbance at 450 nm is measured with a microplate reader. The optical density (OD) values are determined to reflect the viable cell populations from each well[1]. |
Animal experiment: | Mice[1]Xenografted tumor models are prepared by injection of 1×107 22B-cFluc cells suspended in PBS into nude mouse (n=6). After tumors reach a volume of approximately 100 mm3, Sanguinarine (10 mg/kg) is i.v. injected into mice. After injection for 24 h, 48 h and 72 h, mice are given a single i.p. dose of 150 mg/kg D-luciferin and bioluminescence imaging are performed using a Xenogen Lumina II system. The signal intensity in the region of interest is expressed using the Living Image software 4.1. For the anti-tumor therapy studies, one group of tumor-bearing mice (n=6) receive intravenously 10 mg/kg of Sanguinarine every other day throughout the experimental period, while the control group of mice (n=6) receive DMSO only. Tumor growth measurement is calculated[1]. |
References: [1]. Wang Y, Noninvasive bioluminescence imaging of the dynamics of sanguinarine induced apoptosis via activation of reactive oxygen species. Oncotarget. 2016 Apr 19;7(16):22355-67. | |
| Cas No. | 5578-73-4 | SDF | |
| 别名 | 氯化血根碱; Sanguinarin chloride; Sanguinarium chloride; Pseudochelerythrine chloride | ||
| 化学名 | 13-methyl-[1,3]dioxolo[4',5':4,5]benzo[1,2-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium chloride | ||
| Canonical SMILES | C[N+]1=C2C(C=CC3=CC(OCO4)=C4C=C32)=C5C=CC(OCO6)=C6C5=C1.[Cl-] | ||
| 分子式 | C20H14ClNO4 | 分子量 | 367.78 |
| 溶解度 | ≥ 3.68mg/mL in DMSO with gentle warming | 储存条件 | 4°C, protect from light |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.719 mL | 13.5951 mL | 27.1902 mL |
| 5 mM | 0.5438 mL | 2.719 mL | 5.438 mL |
| 10 mM | 0.2719 mL | 1.3595 mL | 2.719 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet