Toggle Nav

WEHI-539

In stock
Catalog No.
A3935
Bcl-xL inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$200.00
In stock
10mg
$245.00
In stock
50mg
$955.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt583.72
Cas No.1431866-33-9
FormulaC31H29N5O3S2
SynonymsWEHI539,WEHI 539
Solubility<1.17 mg/mL in DMSO, <2.44 mg/mL in EtOH, <2.24 mg/mL in H2O
Chemical Name5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[(8E)-8-(1,3-benzothiazol-2-ylhydrazinylidene)-6,7-dihydro-5H-naphthalen-2-yl]-1,3-thiazole-4-carboxylic acid
SDFDownload SDF
Canonical SMILESC1CC2=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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment[1]:

Cell lines

Human colon cancer cell

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 μM, 24h

Applications

Limiting dilution analysis with CSCs that were pre-treated with ABT-737, ABT-199 or WEHI-539 revealed that ABT-737 and WEHI-539 both were sufficient to decrease clonogenic capacity, whereas ABT-199 did not affect clonogenic growth. As WEHI-539 is selective for BCLXL, this points to a dependency of CSCs on BCLXL for survival. Importantly, ABT-737- or WEHI-539-induced loss of clonogenicity could be restored when BCLXL was ectopically overexpressed. When spheroid cultures were treated with ABT-737 or WEHI-539 compounds, CSCs were effectively sensitized toward oxaliplatin and other chemotherapeutic agents.

References:

1. Colak S, Zimberlin CD, Fessler E et al. Decreased mitochondrial priming determines chemoresistance of colon cancer stem cells. Cell Death Differ. 2014 Jul;21(7):1170-7.

Biological Activity

WEHI-539, has high affinity (subnanomolar) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 has a high affinity for BCL-XL (IC50 = 1.1 nM).
Targets BCL-XL          
IC50 1.1 nM          

Quality Control

Chemical structure

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539

Related Biological Data

WEHI-539