WEHI-539 (Synonyms: WEHI539,WEHI 539) |
| カタログ番号GC11921 |
選択的なBcl-xL阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1431866-33-9
Sample solution is provided at 25 µL, 10mM.
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WEHI-539 is a small-molecule inhibitor of BCL XLwith an IC50 value of 1.1 nM [1].
WEHI-539 was designed as a BCL-XLinhibitor with high affinity. It interacted the with the binding groove of BCL-XLwith a 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 cand caspase-3 processing. In BCL-XLoverexpressed 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-539can not kill MEF cells lacking BAK because the cell death mediator BAK is regulated by BCL-XLand MCL-1. [1].
References:
[1] Lessene G, Czabotar P E, Sleebs B E, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.
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