Home Apoptosis Bcl-2 antagonist WEHI-539

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WEHI-539 Bcl-2 antagonist

Cat.No.S7100

WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. This compound has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.
WEHI-539 Bcl-2 antagonist Chemical Structure

Chemical Structure

Molecular Weight: 583.73

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Quality Control

Batch: S710001 DMSO]100 mg/mL]false]]]false]]]false Purity: 99.42%
99.42

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 583.73 Formula

C31H29N5O3S2

 Storage (From the date of receipt)
CAS No. 1431866-33-9 Download SDF Storage of Stock Solutions

Mechanism of Action

Targets/IC50/Ki
Bcl-xL
(Cell-free assay)
1.1 nM
In vitro
WEHI-539 shows good selectivity for BCL-XL. The tight ligand of this compound retains this selectivity (500-fold over BCL-2 and 400-fold over BCL-W, MCL-1 and A1). It kills fibroblasts that lack MCL-1. Thus, this compound not only binds very tightly to BCL-XL, with IC50 and KD values close to or below 1 nM as well as a slow dissociation rate, but also invokes apoptotic responses that depend on BAX, BAK or both; furthermore, its biological activity is related to its binding profile, as elevated amounts of MCL-1, BCL-2 and BCL-W confer marked resistance, and its ability to destroy platelets is a well-validated marker of on-target BCL-XL inhibition. In addition, this chemical induces a preferentially BAK-dependent apoptotic response in MEFs by selectively inhibiting BCL-XL.
Kinase Assay
AlphaScreen assay
The assay buffer (stock 50 mM HEPES and 100 mM NaCl, pH 7.5) is prepared fresh daily and adjusted to 5 mM DTT, casein (0.1 mg/mL sodium salt; aliquots stored at -20 °C) and Tween 20 such that the
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