WEHI-539

The Uses of WEHI-539

WEHI 539 is a selective BCL-XL inhibitor.

Biological Activity

wehi-539 is a small-molecule inhibitor of bclxlwith 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.