1. Apoptosis
  2. Bcl-2 Family

WEHI-539 hydrochloride (Synonyms: WEHI539 hydrochloride; WEHI 539 hydrochloride)

Cat. No.: HY-15607A Purity: 97.85%
Data Sheet SDS Handling Instructions

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

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WEHI-539 hydrochloride Chemical Structure

WEHI-539 hydrochloride Chemical Structure

CAS No. :

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10 mM * 1 mL in DMSO $164 In-stock
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10 mg $150 In-stock
50 mg $520 In-stock
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Description

WEHI-539 hydrochloride 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 hydrochloride 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 (DMSO) 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
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].

References
M.Wt

620.18

Formula

C₃₁H₃₀ClN₅O₃S₂

CAS No.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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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Product Name:
WEHI-539 hydrochloride
Cat. No.:
HY-15607A
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