1. Apoptosis NF-κB Autophagy
  2. IAP NF-κB Apoptosis Autophagy
  3. Embelin

Embelin  (Synonyms: Embelic acid; Emberine; NSC 91874)

Cat. No.: HY-17473 Purity: 98.75%
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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.

Embelin Chemical Structure

Embelin Chemical Structure

CAS No. : 550-24-3

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 42 In-stock
10 mg USD 66 In-stock
50 mg USD 258 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Embelin:

Top Publications Citing Use of Products

    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).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3].

    IC50 & Target[1]

    XIAP

    4.1 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    1.79 μM
    Compound: 5
    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
    [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
    [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]
    In Vitro

    Embelin (Embelic acid) has a minimal effect on normal prostate epithelial and fibroblast cells with low levels of XIAP[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    294.39

    Formula

    C17H26O4

    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C1C(O)=C(CCCCCCCCCCC)C(C(O)=C1)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3969 mL 16.9843 mL 33.9685 mL
    5 mM 0.6794 mL 3.3969 mL 6.7937 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (8.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 98.75%

    References

    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
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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