WEHI-539
Catalogue Number: A3935-APE
| Manufacturer: | Apexbio |
| Physical state: | A solid |
| Type: | Other Inhibitors |
| Alias: | WEHI539,WEHI 539 |
| Shipping Condition: | Blue Ice |
| Unit(s): | 5 mg, 10 mg, 50 mg |
Description
Description: 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.
Additional Text
Storage Note
Store at -20°C
Short Description
Bcl-xL inhibitor,potent and selective
Reagent:Smile String
C1CC2=C(C=C(C=C2)C3=NC(=C(S3)CCCOC4=CC=C(C=C4)CN)C(=O)O)C(=NNC5=NC6=CC=CC=C6S5)C1
Solubility
insoluble in DMSO; insoluble in H2O; insoluble in EtOH
A3935 Datasheet
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