Embelin

製品コードS7025 バッチS702501

印刷

化学情報

Chemical Structure Synonyms Embelic Acid, NSC 91874 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H26O4
分子量 294.39 CAS No. 550-24-3
Solubility (25°C)* 体外 DMSO 59 mg/mL (200.41 mM)
Ethanol 12 mg/mL (40.76 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Human prostate cancer cell lines (PC-3, LNCap), normal human fibroblast cell line WI-38, and humanprostate epithelial cells (PrEC)
濃度 1-64 μM
反応時間 4-5 days
実験の流れ 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.

カスタマーフィードバック

Data from [Data independently produced by , , Leukemia, 2016, 812-822.]

Data from [Data independently produced by , , Antiviral Res, 2018, 158:13-24]

Data from [Data independently produced by , , Inflammation, 2015, 38(4): 1556-1562.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Embelin attenuates lipopolysaccharide-induced acute kidney injury through the inhibition of M1 macrophage activation and NF-κB signaling in mice [ Heliyon, 2023, 9(3):e14006] PubMed: 36938407
Targeting c-IAP1, c-IAP2, and Bcl-2 Eliminates Senescent Glioblastoma Cells Following Temozolomide Treatment [ Cancers (Basel), 2021, 13(14)3585] PubMed: 34298797
SMAC Mimetics Induce Autophagy-Dependent Apoptosis of HIV-1-Infected Resting Memory CD4+ T Cells. [ Cell Host Microbe, 2018, 24(5):689-702] PubMed: 30344003
Aberrant regulation of the Akt signaling network by human cytomegalovirus allows for targeting of infected monocytes [Peppenelli MA Antiviral Res, 2018, 158:13-24] PubMed: 30055197
Porphyromonas gingivalis Differentially Modulates Apoptosome Apoptotic Peptidase Activating Factor 1 in Epithelial Cells and Fibroblasts [Bugueno IM Am J Pathol, 2018, 188(2):404-416] PubMed: 29154960
Regulation of XIAP Turnover Reveals a Role for USP11 in Promotion of Tumorigenesis. [Zhou Z, et al. EBioMedicine, 2017, 15:48-61] PubMed: 28040451
Calcineurin and GSK-3 inhibition sensitizes T-cell acute lymphoblastic leukemia cells to apoptosis through X-linked inhibitor of apoptosis protein degradation. [Tosello V, et al. Leukemia, 2016, 30(4):812-22] PubMed: 26648536
Embelin Reduces Systemic Inflammation and Ameliorates Organ Injuries in Septic Rats Through Downregulating STAT3 and NF-κB Pathways. [Zhou XL, et al. Inflammation, 2015, 38(4):1556-62] PubMed: 25682469

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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