Embelin
Based on 6 publication(s) in Google Scholar
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
For research use only. We do not sell to patients.
- Purity: 99.01%
- CAS No.: 550-24-3
- Formula: C17H26O4
- Molecular Weight:294.39
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Storage:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications Citing Use of MedChemExpress (MCE) Embelin
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WB
Biological Activity
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XIAP 4.1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
1.79 μM
Compound: 5
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Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
|
[PMID: 17125236] |
| A549 | IC50 |
0.21 μM
Compound: 2
|
Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method
Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method
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[PMID: 25765759] |
| A549 | IC50 |
1.47 μM
Compound: 5
|
Cytotoxicity against human A549 cells after 96 hrs by MTT assay
Cytotoxicity against human A549 cells after 96 hrs by MTT assay
|
[PMID: 17125236] |
| Bel-7402 | IC50 |
1.66 μM
Compound: 5
|
Cytotoxicity against human Bel-7402 cells after 96 hrs by MTT assay
Cytotoxicity against human Bel-7402 cells after 96 hrs by MTT assay
|
[PMID: 17125236] |
| BGC-823 | IC50 |
1.69 μM
Compound: 5
|
Cytotoxicity against human BGC-823 cells after 96 hrs by MTT assay
Cytotoxicity against human BGC-823 cells after 96 hrs by MTT assay
|
[PMID: 17125236] |
| CHO | EC50 |
0.421 μM
Compound: 2
|
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
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[PMID: 31721581] |
| CHO | EC50 |
5 μM
Compound: 2
|
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
|
[PMID: 31721581] |
| HCT-8 | IC50 |
1.49 μM
Compound: 5
|
Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay
Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay
|
[PMID: 17125236] |
| HEK293 | EC50 |
0.089 μM
Compound: 2
|
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assay
Agonist activity at recombinant human HA-tagged GPR84 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 60 mins by HTRF assay
|
[PMID: 31721581] |
| HEK293 | EC50 |
0.63 μM
Compound: 2
|
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
|
[PMID: 31721581] |
| Jurkat | IC50 |
20 μM
Compound: Embelin
|
Inhibitory concentration of compound against Jurkat-Vec cells
Inhibitory concentration of compound against Jurkat-Vec cells
|
[PMID: 15115387] |
| LNCaP | IC50 |
5.7 μM
Compound: Embelin
|
Compound was tested for inhibition of LnCap prostate cancer cells
Compound was tested for inhibition of LnCap prostate cancer cells
|
[PMID: 15115387] |
| LNCaP | IC50 |
5.7 μM
Compound: Embelin
|
Inhibitory concentration of compound against growth of LNCaP cells in vitro
Inhibitory concentration of compound against growth of LNCaP cells in vitro
|
[PMID: 15115387] |
| PC-3 | IC50 |
3.7 μM
Compound: Embelin
|
Compound was tested for inhibition of PC-3 prostate cancer cells
Compound was tested for inhibition of PC-3 prostate cancer cells
|
[PMID: 15115387] |
| PC-3 | IC50 |
3.7 μM
Compound: Embelin
|
Inhibitory concentration of compound against growth of PC-3 cells in vitro
Inhibitory concentration of compound against growth of PC-3 cells in vitro
|
[PMID: 15115387] |
| PrEC | IC50 |
20.1 μM
Compound: Embelin
|
Inhibitory concentration of compound against growth of PrEC cells in vitro
Inhibitory concentration of compound against growth of PrEC cells in vitro
|
[PMID: 15115387] |
| PrEC | IC50 |
20.1 μM
Compound: Embelin
|
Selectivity in normal human prostate epithelial cells (PrEC)
Selectivity in normal human prostate epithelial cells (PrEC)
|
[PMID: 15115387] |
| WI-38 | IC50 |
19.3 μM
Compound: Embelin
|
Inhibitory concentration of compound against growth of WI-38 cells in vitro
Inhibitory concentration of compound against growth of WI-38 cells in vitro
|
[PMID: 15115387] |
| WI-38 | IC50 |
19.3 μM
Compound: Embelin
|
Selectivity in normal human fibroblast cell line, WI-38 cells
Selectivity in normal human fibroblast cell line, WI-38 cells
|
[PMID: 15115387] |
Chemical Information
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CAS No. 550-24-3
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Appearance Solid
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Molecular Weight 294.39
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Formula C17H26O4
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Color Yellow to orange
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SMILES
O=C1C(O)=C(CCCCCCCCCCC)C(C(O)=C1)=O
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Synonyms
Embelic acid; Emberine; NSC 91874
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Res
2021 Mar;31(3):291-311. PMID: 33299139 -
Autophagy
XIAP-ULK1-Mediated mitophagy modulates carnitine metabolism to mitigate diabetic kidney disease. [Abstract]2025 Oct 25. PMID: 41139215 -
Sci Adv
In situ protein corona-camouflaged supramolecular assemblies remodel thrombotic microenvironment for improved arterial homeostasis. [Abstract]2025 May 2;11(18):eadu6676. PMID: 40315315 -
Pharmacol Res
Cardamonin retards progression of autosomal dominant polycystic kidney disease via inhibiting renal cyst growth and interstitial fibrosis. [Abstract]2020 May;155:104751. PMID: 32151678 -
Mol Pharm
Construction of SLC16A1/3 Targeted Gallic Acid-Iron-Embelin Nanoparticles for Regulating Glycolysis and Redox Pathways in Cervical Cancer. [Abstract]2023 Sep 4;20(9):4574-4586. PMID: 37307591 -
Mol Neurobiol
Embelin suppresses dendritic cell functions and limits autoimmune encephalomyelitis through the TGF-β/β-catenin and STAT3 signaling pathways. [Abstract]2014 Apr;49(2):1087-101. PMID: 24258405
Embelin purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2014 Apr;49(2):1087-101. [Abstract]
Embelin (EB) promotes TGF-β/β-catenin and inhibits STAT3 signaling in mDCs. DCs are treated with 10, 30, and 60 μM EB to investigate its effect on p-STAT3, TGF-β, β-catenin, and p-GSK-3β signaling (diluted 1:1,000).
Solvent & Solubility
DMSO : ≥ 50 mg/mL (169.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Nikolovska-Coleska Z, et al. Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database. J Med Chem. 2004;47(10):2430-2440. [Content Brief]
[2]. Ahn KS, et al. Embelin, an inhibitor of X chromosome-linked inhibitor-of-apoptosis protein, blocks nuclear factor-kappaB (NF-kappaB) signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Mol Pharmacol. 2007;71(1):209-219. [Content Brief]
[3]. Lee YJ, et al. XIAP inhibitor embelin induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells. Environ Toxicol. 2017;32(11):2371-2378. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3969 mL | 16.9843 mL | 33.9685 mL | 84.9214 mL |
| 5 mM | 0.6794 mL | 3.3969 mL | 6.7937 mL | 16.9843 mL | |
| 10 mM | 0.3397 mL | 1.6984 mL | 3.3969 mL | 8.4921 mL | |
| 15 mM | 0.2265 mL | 1.1323 mL | 2.2646 mL | 5.6614 mL | |
| 20 mM | 0.1698 mL | 0.8492 mL | 1.6984 mL | 4.2461 mL | |
| 25 mM | 0.1359 mL | 0.6794 mL | 1.3587 mL | 3.3969 mL | |
| 30 mM | 0.1132 mL | 0.5661 mL | 1.1323 mL | 2.8307 mL | |
| 40 mM | 0.0849 mL | 0.4246 mL | 0.8492 mL | 2.1230 mL | |
| 50 mM | 0.0679 mL | 0.3397 mL | 0.6794 mL | 1.6984 mL | |
| 60 mM | 0.0566 mL | 0.2831 mL | 0.5661 mL | 1.4154 mL | |
| 80 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0615 mL | |
| 100 mM | 0.0340 mL | 0.1698 mL | 0.3397 mL | 0.8492 mL |