WEHI-539 hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

规格:	98%
分子量:	620.18

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

WEHI-539 hydrochloride 是 Bcl-XL 的选择性抑制剂，IC50 为 1.1 nM。
货号:ajcx11206
CAS:2070018-33-4
分子式:C31H30ClN5O3S2
分子量：620.18
溶解度:≥ 28.55mg/mL in DMSO
纯度：98%
存储：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].

参考文献:
[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]:
Cell lines	Human colon cancer cell
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.
Reaction Conditions	1 μM, 24h
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.
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.