Magnolin - ERK 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMagnolinCat. No.: HY-N1374CAS No.: 31008-18-1分式: CHO分量: 416.46作靶點: ERK作通路: MAPK/ERK Pathway; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (300.15 mM; Need ultrason

2、ic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4012 mL 12.0060 mL 24.0119 mL5 mM 0.4802 mL 2.4012 mL 4.8024 mL10 mM 0.2401 mL 1.2006 mL 2.4012 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以

3、下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.99 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.99 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.99 mM); Clea

4、r solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 MagnolinMagnolia flos (Shin-Yi) 的主 成分，靶向作于ERK1 和 ERK2，IC50s 分別為 87 nM 和 16.5nM，從抑制Ras/ERKs/RSK2信號通路。IC50 & Target ERK2 ERK116.5 nM (IC50) 87 nM (IC50)體外研究 Magnolin is a natural compound abundantly found in Magnolia flo

5、s, which has been traditionally used inoriental medicine to treat headaches, nasal congestion and anti-inflammatory reactions. Magnolin targets theactive pockets of ERK1 and ERK2, which are important signaling molecules in cancer cell metastasis.Magnolin inhibits NF-B transactivation activity by sup

6、pressing the ERKs/RSK2 signaling pathway. Magnolininhibits the production of tumor necrosis factor- (TNF-) and prostaglandin E2 (PGE2) by inhibitingextracellular signal-regulated kinases (ERKs), which are key signaling molecules in the regulation of cellproliferation, transformation and cancer cell

7、metastasis. JB6 Cl41 cell migration enhanced by EGF treatmentis dramatically suppressed by Magnolin treatment in a dose-dependent manner. Magnolin inhibitsERK1/2/RSK2 signaling-mediated IB phosphorylation at Ser32, resulting in the inhibition of NF-Bactivation and cell migration 1.PROTOCOLCell Assay

8、 1 JB6 Cl41 (7104), A549 (7104) and NCI-H1975 (7104) cells, and RSK2+/+ (7104) and RSK2-/- (7104)MEFs are seeded into culture-inserts and cultured overnight. The cells are treated with mitomycin-C (10 g/mL) for 2 h, and the culture-inserts are removed to offer a cell-free gap. The cells are treated

9、with theindicated doses of Magnolin (15, 30, and 60 M) either in the presence or absence of EGF for 12 or 24 h,and cell migration is observed under a light microscope. The migrated area is measured using the Image Jcomputer software program. To measure the Magnolin effect on cancer cell invasion, a

10、matrigel-coatedinvasion chamber is used. Briefly, A549 or NCI-H1975 (2.5104) cells are seeded into an insert chamber withFBS-free media supplemented with the indicated doses of Magnolin(15, 30, and 60 M), and cultured in 24-well plates supplemented with complete media for the appropriate time period

11、. The cells are fixed with 4 %formaldehyde, permeabilized with methanol and stained with crystal violet. The stained cells are observedunder a light microscope and those that have migrated are counted 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug8;15:576.McePdfHeightCaution: Product h