WEHI-539
WEHI-539 Basic information
- Product Name:
- WEHI-539
- Synonyms:
-
- WEHI-539
- (E)-5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazono)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid
- WEHI-539 ( CT-WE539)
- 5-[3-[4-(Aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-4-thiazolecarboxylic acid
- (E)-5-(3-(4-(Aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazono)-5,6,7,8-tetr
- CS-1739
- WEHI539;WEHI 539
- 4-Thiazolecarboxylic acid, 5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-
- CAS:
- 1431866-33-9
- MF:
- C31H29N5O3S2
- MW:
- 583.72
- Mol File:
- 1431866-33-9.mol
WEHI-539 Chemical Properties
- Boiling point:
- 827.6±75.0 °C(Predicted)
- Density
- 1.44±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in DMSO; insoluble in H2O; insoluble in EtOH
- form
- solid
- pka
- 10.24±0.20(Predicted)
WEHI-539 Usage And Synthesis
Uses
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].
target
BCL-XL
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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