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  3. WEHI-539 hydrochloride

WEHI-539 hydrochloride 

Cat. No.: HY-15607A Purity: 98.16%
Handling Instructions

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

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

WEHI-539 hydrochloride Chemical Structure

WEHI-539 hydrochloride Chemical Structure

CAS No. : 2070018-33-4

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10 mM * 1 mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    WEHI-539 hydrochloride purchased from MCE. Usage Cited in: Int J Cancer. 2018 Feb 1;142(3):584-596.

    Evaluation of PARP protein cleavage in Mneo and MXL90 cells after treatment for 24h with 20 μM NSC 119875, in presence of increasing doses of the specific Bcl-xL inhibitor WEHI-539.

    WEHI-539 hydrochloride purchased from MCE. Usage Cited in: Blood. 2014 Dec 4;124(24):3587-96.

    CD41+ or CD41 cells are treated with DMSO as a vehicle control or a BCL-xL inhibitor (WEHI-539; 0.2, 0.4, and 0.8 μM) on OP9 stromal cells in the presence of THPO for 7 days. The number of viable cells is counted.

    WEHI-539 hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2018 May 25;9(40):26046-26063.

    Representative images of Hoechst/PI merged channels for WEHI-539 treatment in MCF7-pSFFV cell line.

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    Description

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

    IC50 & Target[1]

    Bcl-xL

    1.1 nM (IC50)

    In Vitro

    WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL. WEHI-539 augments NSC 241240 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].

    Molecular Weight

    620.18

    Formula

    C₃₁H₃₀ClN₅O₃S₂

    CAS No.

    2070018-33-4

    SMILES

    OC(C1=C(CCCOC2=CC=C(CN)C=C2)SC(C3=CC4=C(CCC/C4=N\NC5=NC(C=CC=C6)=C6S5)C=C3)=N1)=O.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (80.62 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6124 mL 8.0622 mL 16.1244 mL
    5 mM 0.3225 mL 1.6124 mL 3.2249 mL
    10 mM 0.1612 mL 0.8062 mL 1.6124 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.03 mM); Suspended solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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 NSC 241240 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

    Purity: 98.16%

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    Keywords:

    WEHI-539WEHI539WEHI 539Bcl-2 FamilyInhibitorinhibitorinhibit

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