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Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $50 | In Stock | |
25 mg | $85 | In Stock | |
50 mg | $160 | In Stock | |
100 mg | $314 | In Stock | |
1 mL x 10 mM (in DMSO) | $50 | In Stock |
Description | Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM). |
Targets&IC50 | X linked:4.1 μM |
In vitro | Embelin from the Japanese Ardisia herb is a small-molecular inhibitor that binds to the XIAP BIR3 domain with which Smac and caspsase-9 bind. Embelin inhibits cell growth of both PC-3 and LNCap cells in a dose-dependent manner, with IC50 values of 3.7 and 5.7 μM. While, the toxicity of Embelin in normal PrEC and in WI-38 cells is much lower with IC50 values of 20.1 μM and 19.3 μM. Treatment of PC-3 cells with 25 and 50 μM of embelin for 48 h, 30% and 75% of cells undergo apoptosis, representing approximately 3-and 9-fold increase as compared to untreated cells. [1] Embelin also potently suppresses the biosynthesis of eicosanoids by selective inhibition of 5-lipoxygenase (5-LO) and Microsomal prostaglandin E2 synthase-1 (mPGES-1) with IC50 = 0.06 and 0.2 mM, respectively. [2] |
Kinase Assay | Fluorescence Polarization Competitive Binding Assay: Fluorescence polarization experiments are performed in Dynex 96-well, black, round-bottom plates. A 5 μL sample of Embelin dilutions in DMSO, and preincubated XIAP BIR3 protein (0.06 μM) and the N terminus of a Smac peptide (SM7F) (0.01 μM) in the assay buffer are added to 96-well plates to produce a final volume of 125 μL. For each assay, the bound peptide control containing XIAP BIR3 protein and SM7F (equivalent to 0% inhibition) and free peptide control containing only free SM7F (equivalent to 100% inhibition) were included. The plates were mixed and incubated at room temperature for 3 h to reach equilibrium. |
Cell Research | Cell growth is determined by the MTT-based assay using Cell Proliferation Reagent WST-1 according to the manufacturer's instruction. Cells (5000 cells/well) are grown in medium with 10% FBS, and various concentrations of Embelin are added to the cells. Four to five days later, WST-1 is added to each well and incubated for 1-3 h at 37 °C. Absorbance is measured with a plate reader at 450 nm with correction at 650 nm.(Only for Reference) |
Alias | NSC 91874, Emberine, Embelic acid |
Molecular Weight | 294.39 |
Formula | C17H26O4 |
Cas No. | 550-24-3 |
Smiles | CCCCCCCCCCCC1=C(O)C(=O)C=C(O)C1=O |
Relative Density. | 1.131 g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 2.9 mg/mL (10 mM)), Heating is recommended. DMSO: 29.4 mg/mL (100 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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