Home Apoptosis Antineoplastic and Immunosuppressive Antibiotics inhibitor - IAP inhibitor Embelin For research use only.

Embelin

Synonyms: Embelic Acid, NSC 91874

Embelin (Embelic Acid, NSC 91874), a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.

Embelin Chemical Structure

Embelin Chemical Structure

CAS No. 550-24-3

Purity & Quality Control

Batch: S702501 DMSO]59 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false Purity: 100.0%
100.0

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Biological Activity

Description Embelin (Embelic Acid, NSC 91874), a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.
Targets
5-LO [2]
(Cell-free assay)		 mPGES-1 [2]
(Cell-free assay)		 XIAP [1]
(Cell-free assay)
0.06 μM 0.2 μM 4.1 μM
In vitro
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 lines Human prostate cancer cell lines (PC-3, LNCap), normal human fibroblast cell line WI-38, and humanprostate epithelial cells (PrEC)
Concentrations 1-64 μM
Incubation Time 4-5 days
Method 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.

Chemical Information & Solubility

Molecular Weight 294.39 Formula

C17H26O4
CAS No. 550-24-3 SDF Download Embelin SDF
Smiles CCCCCCCCCCCC1=C(C(=O)C=C(C1=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (200.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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