WEHI-539 hydrochloride
Modify Date: 2024-01-02 19:07:02
WEHI-539 hydrochloride structure
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Common Name | WEHI-539 hydrochloride | ||
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| CAS Number | 2070018-33-4 | Molecular Weight | 620.18 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C31H29N5O3S2·HCl | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of WEHI-539 hydrochlorideWEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM. |
| Name | WEHI-539 hydrochloride |
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| Description | WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM. |
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| Related Catalog | |
| Target |
Bcl-xL:1.1 nM (IC50) |
| 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]. |
| Cell Assay | 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 |
| Molecular Formula | C31H29N5O3S2·HCl |
|---|---|
| Molecular Weight | 620.18 |
| Storage condition | -20℃ |