WEHI-539 hydrochloride
A selective Bcl-xL inhibitor
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包装价格促销价数量
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5mg￥1800.001440.00- +
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10mg￥2300.001840.00- +
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50mg￥8387.006710.00- +
- 货号: ajcx11206
- CAS: 2070018-33-4
- 别名:
- 分子式: C31H30ClN5O3S2
- 分子量: 620.18
- 纯度: ＞98%
- 溶解度: 100 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- 储存: Store at -20°C
- 库存: 现货
Background
WEHI-539 hydrochloride is a small-molecule inhibitor of BCL XL with IC50 value of 1.1 nM [1].
WEHI-539 was designed as a BCL-XL inhibitor with high affinity. It interacted with the binding groove of BCL-XL with Kd value of 0.6 nM. In MEF cells lacking MCL-1, WEHI-539 induced apoptosis which was evidenced by the release of mitochondrial cytochrome c and caspase-3 processing. In BCL-XL overexpressed MEF cells, WEHI-539 showed EC50 value of 0.48 μM. WEHI-539 also significantly induced apoptosis of the platelets purified from mice. Besides that, WEHI-539 cannot kill MEF cells lacking BAK because the cell death mediator BAK is regulated by BCL-XL and MCL-1. [1].
Reference:
[1].? Lessene G, Czabotar PE, Sleebs BE, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.
Protocol
| Cell experiment[1]: | |
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Cell lines |
Human colon cancer cell |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μM, 24h |
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Applications |
Limiting dilution analysis with CSCs that were pre-treated with ABT-737, ABT-199 or WEHI-539 revealed that ABT-737 and WEHI-539 both were sufficient to decrease clonogenic capacity, whereas ABT-199 did not affect clonogenic growth. As WEHI-539 is selective for BCLXL, this points to a dependency of CSCs on BCLXL for survival. Importantly, ABT-737- or WEHI-539-induced loss of clonogenicity could be restored when BCLXL was ectopically overexpressed. When spheroid cultures were treated with ABT-737 or WEHI-539 compounds, CSCs were effectively sensitized toward oxaliplatin and other chemotherapeutic agents. |
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参考文献: 1. Colak S, Zimberlin CD, Fessler E et al. Decreased mitochondrial priming determines chemoresistance of colon cancer stem cells. Cell Death Differ. 2014 Jul;21(7):1170-7. |
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