WEHI-539 hydrochloride |
| カタログ番号GC13317 |
WEHI-539 塩酸塩は、Bcl-XL の選択的阻害剤であり、IC50 は 1.1 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070018-33-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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