Emodin-Frangula-emodin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEmodinCat. No.: HY-14393CAS No.: 518-82-1Synonyms: Frangula emodin分式: CHO分量: 270.24作靶點(diǎn): Casein Kinase; Autophagy作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 9.4 mg/mL (34.78 mM; Need ultrasonic and warming)H2O : 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (4.63 mM); Suspended solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1.25 mg/mL (4.63 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.Med

3、ChemEBIOLOGICAL ACTIVITY物活性 Emodin種譜抗癌劑。Emodin 抑制蛋激酶 CKII 活性，IC50 為 2 M。IC50 & Target CKII2 M (IC50)體外研究 Emodin, an anthraquinone derivative, selectively inhibits casein kinase II(CKII), a Ser/Thr kinase, as acompetitive inhibitor. Emodin inhibits CKII activity with IC50 of 2 M, which is two to thre

4、e orders ofmagnitude lower than those against the other kinases. Enzyme kinetic assays show that Emodin inhibits CKIIactivity as acompetitive inhibitor against ATP with Ki of 7.2 M 1. Emodin is a broad-spectrum inhibitoryagent of cancer cells, including leukemia, lung cancer, human tongue squamous c

5、ancer, colon cancer,gallbladder cancer, pancreatic cancer, breast cancer, human cervical cancer and hepatic carcinoma cells.Emodin inhibits A549, HepG2, OVCAR-3, HeLa and Madin-Darby Canine Kidney (MDCK) cells with IC50 of19.54, 12.79, 25.82, 12.14 and 5.81 g/mL. The anticancer mechanisms of Emodin

6、are involved in manybiological pathways, such as casein kinase II and ERK1/2 2. Emodin is applied as a Reactive oxygenspecies (ROS) generator in combination with cisplatin in T24 and J82 human bladder cancer cells. Emodinkills T24 and J82 cells in the dose-dependent and time-dependent manner, and it

7、 is less toxic to HCV-29cells. The concentration of 20 and 15 M is selected as appropriate doses for investigating chemotherapeuticsensitivity of T24 and J82 cells at 24 h, respectively 3.體內(nèi)研究 Mice treated with Emodin (50 mg/kg) and Cisplatin (1 mg/kg) have significantly smaller tumors than thosefro

8、m the other groups. In addition, no notable differences on the body weight loss are observed amonggroups and no obvious necrosis and abnormity are observed in the sections of liver, kidney and heart. Theseresults demonstrate that Emodin/cisplatin co-treatment can significantly suppress tumor growth

9、in vivo withno distinct side effects. Consistent with in vitro experiment, TUNEL assay shows that Emodin/cisplatincombination significantly increased cell apoptosis in xenograft tumors. Emodin/Cisplatin co-treatment groupalso has lower MRP1 expression than the other groups 3.PROTOCOLCell Assay 3 The

10、 T24 human bladder cancer cells, the HCV-29 normal bladder epithelial cells and J82 human bladdercancer cells are are cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum at 37C in ahumidified atmosphere containing 5 % CO2. Cells are seeded in 96-well plates with 2104 cells per wel

11、l. Thecells are incubated with Emodin for 24 h at different concentrations (0, 5, 10, 20, 30, 40, 50, 60, 70 M) andchose the critical concentration (20 M) treated with cells for 0, 6, 12, 24, 48, 72, 96 h. The cells areincubated with cisplatin for 24 h at different concentrations (0, 0.5, 1.0, 1.5,

12、2.0, 2.5, 3.0 g/mL). MTT assayis used to analyze the cell viability. Cells are treated with drugs for 24 h and apoptotic rates are assessedwith flow cytometry using AnnexinV-fluorescein isothiocyanate (AnnexinV-FITC)/propidium iodide (PI) kit.Samples are prepared according to the manufacturers instr

13、uction and analyzed by a flow cytometry (FCM)Calibur 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Mice 3Administration 3 3106 T24 cells are harvested, washed, and resuspended in serum-free opt

14、imum medium and then injectedsubcutaneously into 6-week old BALB/c-nu/nu mice (n=8 mice per group). Three days after inoculation, themice are intraperitoneally administered with PBS, Emodin (50 mg/kg), Cisplatin (1 mg/kg), orEmodin/cisplatin every two days. On day 18, every mouse is sacrificed. Afte

15、r body weight measurement,tumors are isolated, weighted and fixed in 4 % paraformaldehyde (PFA). Hearts, livers and kidneys arestained with Hematoxylin & Eosin to determine the systemic toxicity. Terminal deoxynucleotidyltransferase(TdT)-mediated dUTP nick end label (TUNEL) assay is performed on par

16、aformaldehyde-fixed andparaffin-embedded tumor sections.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yim H, et al. Emodin, an anthraquinone derivative isolated from the rhizomes of Rheum palmatum, selectively inhibits the activity ofcase

17、in kinase II as a competitive inhibitor. Planta Med. 1999 Feb;65(1):9-13.2. Xing JY, et al. Antitumor Effects and Mechanism of Novel Emodin Rhamnoside Derivatives against Human Cancer CellsIn Vitro. PLoSOne. 2015 Dec 18;10(12):e0144781.3. Li X, et al. Emodin enhances cisplatin-induced cytotoxicity in human bladder cancer cells through ROS elevat