In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonising its prosurvival activity. This compound has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.
Targets
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 Apoptosis 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 Apoptosis response in MEFs by selectively inhibiting BCL-XL.
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
Wild-type (WT), mcl-1−/−, bcl-2−/− or bcl-x−/− MEFs were treated with 10 μM WEHI-539 or ABT-737 for 1 h and fractionated into mitochondrial-enriched (pellet) and cytosolic (soluble) fractions, which were subjected to SDS-PAGE and immunoblotted with antibody against cytochrome c (anti-cyt c); HSP70 was used as a loading control.
References
https://pubmed.ncbi.nlm.nih.gov/23603658/
Sellecks WEHI-539 Has Been Cited by 11 Publications
Multi-selective RAS(ON) Inhibition Targets Oncogenic RAS Mutations and Overcomes RAS/MAPK-Mediated Resistance to FLT3 and BCL2 Inhibitors in Acute Myeloid Leukemia
[ bioRxiv, 2025, 2025.06.10.658786]
Allosteric SHP2 inhibition increases apoptotic dependency on BCL2 and synergizes with venetoclax in FLT3- and KIT-mutant AML
[ Cell Rep Med, 2023, 4(11):101290]
Exploiting ulnerabilities induced b recurrent mutations in chondrosarcoma and giant cell tumour of bone: therapeutic targeting of the altered epigenome and be
[ Leiden University
The Netherlands, 2023, ]
BCL-XL is crucial for progression through the adenoma-to-carcinoma sequence of colorectal cancer
[ Cell Death Differ, 2021, 10.1038/s41418-021-00816-w]
Identification des voies de signalisations impliquées dans l'activité pro-apoptotique du récepteur à dépendance UNC5B
[ HAL open science, 2021, version 1]
Intracellular BH3 Profiling Reveals Shifts in Antiapoptotic Dependency in Human B Cell Maturation and Mitogen-Stimulated Proliferation
[Dai J J Immunol, 2018, 200(5):1727-1736]
Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer
[Goodwin CM Cell Death Differ, 2015, 22(12):2098-106]
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
