Catalog No.S7025 Synonyms: Embelic Acid, NSC 91874

For research use only.

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

CAS No. 550-24-3

Selleck's Embelin has been cited by 7 Publications

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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.
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

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]

Protocol (from reference)

Kinase Assay:[1]
  • 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:[1]
  • 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.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 59 mg/mL
(200.41 mM)
Ethanol 12 mg/mL
(40.76 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 294.39


CAS No. 550-24-3
Storage 3 years -20°C powder
2 years -80°C in solvent

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