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: 550-24-3

Selleck's Embelin has been cited by 8 Publications

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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 lnformation & 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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