Sanguinarine-chloride-Pseudochelerythrine-chloride-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESanguinarine chlorideCat. No.: HY-N0052ACAS No.: 5578-73-4Synonyms: Pseudochelerythrine chloride; Sanguinarium chloride分式: CHClNO分量: 367.78作靶點: Apoptosis; Autophagy作通路: Apoptosis; Autophagy儲存式: 4C, protect from light* In solvent

2、 : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.5 mg/mL (1.36 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.5 mg/mL (1.36 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGI

3、CAL ACTIVITY物活性 Sanguinarine chloride種來 于 Sanguinaria Canadensis 的物堿，可通過激活活性氧 (ROS) 的產(chǎn)來刺激細胞凋亡。Sanguinarine 誘導的細胞凋亡與 JNK 和 NF-B 的活化有關。IC50 & Target Apoptosis 1體外研究 Sanguinarine (SANG)-induced apoptosis is associated with the activation of JNK and NF-B signalpathways.To determine the effects of Sangui

4、narine on cell viability, 22B-cFluc cells are stimulated withdifferent concentrations of Sanguinarine for 24 h, and then a CKK-8 assay is performed. The treatment withSanguinarine decreases the proliferation of 22B cells in a dose-dependent manner. Meanwhile, the cytosolicextracts of 22B-cFluc cells

5、 treated with different dose of Sanguinarine are measured to detect cellularcaspase-3 activity using Ac-DEVD-pNA, which is a validated caspase-3 substrate. The absorbance at 450nm increases in a dose-dependent manner, indicating increased caspase-3 activity stimulated bySanguinarine 1.體內(nèi)研究 To evalua

6、te the apoptosis induced by Sanguinarine (SANG) in vivo, 22B-cFluc cells are inoculatedsubcutaneously into one flank of nude mice and xenograft models are allowed to establish. Mice are treatedintravenously with 10 mg/kg of Sanguinarine. At 24, 48 and 72 h after treatment, bioluminescent imaging isp

7、erformed after i.p. injection of mice with 150 mg/kg of D-luciferin substrate. Sanguinarine treatment inducesan obvious increase of luminescent signal as early as 48 h after initial treatment. A sustained bioluminescentimaging (BLI) intensity increased is observed throughout the course of experiment

8、. At 72 h after treatment,the tumors are collected and subjected to TUNEL staining for evaluating apoptosis. Compared with thecontrol tumors, the group treated with Sanguinarine exhibits significantly more cell apoptosis, indicated by theincreased green signals from the sporadic apoptotic cells 1.PR

9、OTOCOLKinase Assay 1 The caspase-3 activity is measured using a caspase-3 activity assay kit. Briefly, the cells treated by differentconcentrations of Sanguinarine (0.5 M, 1 M, 2 M, 4 M) or control DMSO are collected, washed andlysed in a lysis buffer for 30 min on ice. The supernatants are then col

10、lected by centrifuging at 1,2000 rpm for10 min. The Ac-DEVD-pNA (2 mM) is added to each sample and incubated at 37C for 1 h. The opticaldensity (OD) of each sample is finally quantified at a wavelength of 405 nm using a spectrophotometer. Thep-NA standard is used to calibrate the caspase-3 activity

11、of each sample 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 The cell viability of Sanguinarine is determined by CCK-8 assay using a cell counting kit-8. Briefly, 22B-cFluccells are seeded in a 96-well plate (5103 cells/well) and treate

12、d with different concentrations ofSanguinarine (0.5 M, 1 M, 2 M, 4 M) for 24 h. Then 10 mL CKK-8 is added to each well for 4 h and theabsorbance at 450 nm is measured with a microplate reader. The optical density (OD) values are determinedto reflect the viable cell populations from each well 1.MCE h

13、as not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 12/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration 1 Xenografted tumor models are prepared by injection of 1107 22B-cFluc cells suspended in PBS into nudemouse (n=6). After tumors reac

14、h 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 intensityin the region of

15、 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 daythroughout the experimental period, while the control group of mice (n=6) receive DMSO only. Tumor growthmeasurement is calculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang Y, Noninvasive bioluminescence imaging of the dynamics of sanguinarine induced apoptosis via activation of reactive oxygenspecies.