1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis Autophagy
  2. JAK STAT Apoptosis Autophagy
  3. Brevilin A

Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.

For research use only. We do not sell to patients.

CAS No. : 16503-32-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Brevilin A:

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
Flow Cytometry
Cell Migration/Invasion Assay
WB
Histological Imaging/Staining

    Brevilin A purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2024 Jan;23(1):70-82.  [Abstract]

    Effect of Brevilin A a treatment and ZEB2-interfering lentivirus on SW480 cell viability using the CCK-8 assay.

    Brevilin A purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2024 Jan;23(1):70-82.  [Abstract]

    Flow cytometry was performed to analyze the percentage of early and late apoptosis treated with Brevilin A.

    Brevilin A purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2024 Jan;23(1):70-82.  [Abstract]

    Effect of Brevilin A and LV-ZEB2 on SW480 cell migration was analyzed by the wound healing assay.

    Brevilin A purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2024 Jan;23(1):70-82.  [Abstract]

    Representative gel blot images of p-STAT3, STAT3, and ZEB2 treated with Brevilin A.

    Brevilin A purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2024 Jan;23(1):70-82.  [Abstract]

    HE staining was performed to observe the pathological changes of colonic tissue treated with Brevilin A (10 mg/kg, i.p.).

    View All JAK Isoform Specific Products:

    View All STAT Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy[1][2].

    IC50 & Target[1]

    STAT3

    10.6 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    > 10 μM
    Compound: 17
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33533247]
    HeLa IC50
    9.2 μM
    Compound: 17
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33533247]
    HepG2 IC50
    > 10 μM
    Compound: 17
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33533247]
    In Vitro

    Brevilin A (1-20 μM; 24 h) inhibits STAT3 signaling in a dose dependent manner[1].
    Brevilin A (0-50 μM; 24-72 h) inhibits the proliferation of NPC cells[2].
    Brevilin A (10 μM; 24 and 48 h) induces DU145 and MDA-MB-468 apoptosis after 24 h treatment[1].
    Brevilin A (12.5 and 25 μM; 24 h) blocks STAT3 tyrosine 705 phosphorylation in A549R cells[1].

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

    Cell Viability Assay[1]

    Cell Line: A549R cells
    Concentration: 1-20 µM
    Incubation Time: 24 hours
    Result: Exhibited STAT3 signaling inhibition in a dose dependent manner with IC50 value of 10.6 µM.

    Cell Proliferation Assay[2]

    Cell Line: CNE-2 cells
    Concentration: 0-50 μM
    Incubation Time: 24, 48, and 72 hours
    Result: Showed IC50 values in CNE-2 cells with treatment times of 24, 48, and 72 h of 7.93, 2.60, and 22.26 µM, respectively.

    Apoptosis Analysis[1]

    Cell Line: DU145 and MDA-MB-468 cells
    Concentration: 10 µM
    Incubation Time: 24 and 48 hours
    Result: Decreased c-Myc and CyclinD1 after 24 h and 48 h treatment, increased cleaved PARP after 24 h treatment.

    Western Blot Analysis[1]

    Cell Line: A549R cells
    Concentration: 12.5 and 25 µM
    Incubation Time: 24 hours
    Result: Inhibits STAT3 phosphorylation in A549R cells.
    In Vivo

    Brevilin A (oral gavage; 10 and 20 mg/kg; once daily; 16 d) inhibits CNE-2 xenograft tumor growth, and inhibits PI3K/AKT and STAT3 signaling in vivo[2].

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

    Animal Model: Male BALB/c nude mice injected with CNE-2 cells[2]
    Dosage: 10 and 20 mg/kg
    Administration: Oral gavage; 10 and 20 mg/kg; once daily; 16 days
    Result: Decreased average tumor volumes and weights treated with 20 mg/kg by 36.3% and 46.0%, respectively, compared to vehicle control.
    Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses.
    Molecular Weight

    346.42

    Formula

    C20H26O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C/C=C(C)\C(O[C@H]1[C@@]([C@@H]2C)([H])[C@@](OC2=O)([H])C[C@@H](C)[C@@]3([H])[C@]1(C(C=C3)=O)C)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (288.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8867 mL 14.4333 mL 28.8667 mL
    5 mM 0.5773 mL 2.8867 mL 5.7733 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. 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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 10 mg/mL (28.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 6.25 mg/mL (18.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 1.67 mg/mL (4.82 mM); Clear solution; Need ultrasonic

    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).
    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: 99.86%

    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. 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 2.8867 mL 14.4333 mL 28.8667 mL 72.1667 mL
    5 mM 0.5773 mL 2.8867 mL 5.7733 mL 14.4333 mL
    10 mM 0.2887 mL 1.4433 mL 2.8867 mL 7.2167 mL
    15 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8111 mL
    20 mM 0.1443 mL 0.7217 mL 1.4433 mL 3.6083 mL
    25 mM 0.1155 mL 0.5773 mL 1.1547 mL 2.8867 mL
    30 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4056 mL
    40 mM 0.0722 mL 0.3608 mL 0.7217 mL 1.8042 mL
    50 mM 0.0577 mL 0.2887 mL 0.5773 mL 1.4433 mL
    60 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
    80 mM 0.0361 mL 0.1804 mL 0.3608 mL 0.9021 mL
    100 mM 0.0289 mL 0.1443 mL 0.2887 mL 0.7217 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    Help & FAQs
    • 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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Requested Quantity *

    Applicant Name *

     

    Salutation

    Email Address *

     

    Phone Number *

    Department

     

    Organization Name *

    City

    State

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Brevilin A
    Cat. No.:
    HY-N2959
    Quantity:
    MCE Japan Authorized Agent: