1. Apoptosis
  2. Bcl-2 Family

WEHI-539 

Cat. No.: HY-15607
Handling Instructions

WEHI-539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.

For research use only. We do not sell to patients.
WEHI-539 Chemical Structure

WEHI-539 Chemical Structure

CAS No. : 1431866-33-9

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Other In-stock Forms of WEHI-539:

Other Forms of WEHI-539:

    WEHI-539 purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Jan;24(1):111-119.

    BCL-XL-BIK complexes can be dissociated using the BCL-XL-inhibitor WEHI-539.
    • Biological Activity

    • Protocol

    • Technical Information

    • References

    Description

    WEHI-539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.

    IC50 & Target

    IC50: 1.1 nM (Bcl-XL)[1]

    In Vitro

    WEHI-539 is a selective inhibitor of Bcl-XL. WEHI-539 augments Carboplatin induced caspase 3/7 activity, PARP cleavage and annexin V labelling. WEHI-539 as a single agent causes noticeable PARP cleavage in Ovcar-4 (5 μM in Ovcar-4.) and Ovsaho (1 μM in Ovsaho) cells[2].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.7132 mL 8.5658 mL 17.1315 mL
    5 mM 0.3426 mL 1.7132 mL 3.4263 mL
    10 mM 0.1713 mL 0.8566 mL 1.7132 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    WEHI-539 (Medchem Express, NJ, USA) is dissolved in DMSO (20 mM) and stored, and then diluted with appropriate media before use[2].

    Ovcar-8, Ovcar-3, Ovcar-4 and Ovsaho cells are grown in the RPMI, Igrov-1, Cov-362 and Cov-318 cells are grown in DMEM and Fuov-1 cells are grown in DMEM/F-12 nutrient mixture. ABT-737, ABT-199 and WEHI-539 (Medchem Express, NJ, USA), are prepared as a 20 mM solution in DMSO. For cell growth assays, cells are plated in 96 wells plate (5,000 cells/well for all cell lines except Ovcar-8 which is plated at a density of 2,500 cells/well). The next day, cells are treated with drugs. After 72 h the culture medium is removed and the cells are fixed with 100 μL of cold 10 % Trichloroacetic acid (TCA), incubated on ice for 30 min and stained with 0.4 % sulforhodamine B (SRB). The data are analysed by using Graphpad Prism 4 software. Non-linear regression is used to fit a four parameters Hill equation. For drug combinations studies the cells are exposed simultaneously to a range of concentrations of carboplatin combined with fixed concentration of BH3 mimetics that is expected from the single agent studies to cause 5 % growth inhibition: ABT-737, 1 μM in Ovcar-8, Ovcar-3 and Igrov-1, 2 μM in Ovcar-4 and Ovsaho and 6 μM in Cov-362; ABT-199, 1 μM in Ovcar-4, 2 μM in Ovcar-3, Igrov-1, Cov-362 and Ovsaho and 3 μM in Ovcar-8; WEHI-539, 0.2 μM in Igrov-1, 0.3 μM in Ovcar-8, 1 μM in Ovcar-3 and Ovsaho, 3.1 μM in Cov-362 and 5 μM in Ovcar-4. Surviving cell number is assessed by SRB staining. A combination index (CI) is calculated[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    583.72

    Formula

    C₃₁H₂₉N₅O₃S₂

    CAS No.

    1431866-33-9

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    WEHI-539
    Cat. No.:
    HY-15607
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