WEHI-539 hydrochloride
Based on 30 publication(s) in Google Scholar
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 2070018-33-4
- Formula: C31H30ClN5O3S2
- Molecular Weight:620.18
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) WEHI-539 hydrochloride
More- Nature. 2017 Nov 9;551(7679):247-250. [Abstract]
- Cell. 2014 Dec 18;159(7):1549-62. [Abstract]
- Nat Biotechnol. 2018 Feb;36(2):179-189. [Abstract]
- Immunity. 2024 Jun 11;57(6):1289-1305.e9. [Abstract]
- Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]
- Blood. 2014 Dec 4;124(24):3587-96. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2016 Mar 9:7:10916. [Abstract]
- Nat Chem Biol. 2022 Jun;18(6):615-624. [Abstract]
- Cell Death Differ. 2017 Jan;24(1):111-119. [Abstract]
- Cell Death Differ. 2014 Jul;21(7):1170-7. [Abstract]
- Cell Death Dis. 2023 Oct 28;14(10):705. [Abstract]
- Pharmacol Res. 2023 Jan:187:106628. [Abstract]
- Cell Death Dis. 2018 Jan 19;9(2):42. [Abstract]
- Cell Death Dis. 2017 Dec 13;8(12):3216. [Abstract]
- Clin Cancer Res. 2019 Dec 1;25(23):7139-7150. [Abstract]
- Acta Pharmacol Sin. 2024 Nov;45(11):2420-2431. [Abstract]
- Cell Rep. 2023 Mar 30;42(4):112324. [Abstract]
- Mol Cancer Ther. 2025 Jul 10. [Abstract]
- Breast Cancer Res Treat. 2019 Feb;173(3):585-596. [Abstract]
- J Ovarian Res. 2016 Apr 14:9:25. [Abstract]
- Int J Cancer. 2018 Feb 1;142(3):584-596. [Abstract]
- Oncol Rep. 2019 Dec;42(6):2416-2425. [Abstract]
- Am J Cancer Res. 2019 Dec 1;9(12):2580-2598. [Abstract]
- Malays Appl Biol. (2020) 49(1): 193-197.
- bioRxiv. 2023 Aug 5.
- University of Michigan. 2020 May.
- Harvard University. 2019 Dec.
- Oncotarget. 2018 May 25;9(40):26046-26063. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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IF
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WB
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Cell Proliferation/Viability Assay
Biological Activity
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Bcl-xL 1.1 nM (IC50) |
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL. WEHI-539 augments NSC 241240 induced caspase 3/7 activity, PARP cleavage and annexin V labelling. WEHI-539 as a single agent causes noticeable PARP cleavage in Ovcar-4 (5 μM in Ovcar-4.) and Ovsaho (1 μM in Ovsaho) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2070018-33-4
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Appearance Solid
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Molecular Weight 620.18
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Formula C31H30ClN5O3S2
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Color Light yellow to light brown
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SMILES
OC(C1=C(CCCOC2=CC=C(CN)C=C2)SC(C3=CC4=C(CCC/C4=N\NC5=NC(C=CC=C6)=C6S5)C=C3)=N1)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (30)
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Journal Impact Factor
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Most Recent
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Nature
2017 Nov 9;551(7679):247-250. PMID: 29088702 -
Cell
2014 Dec 18;159(7):1549-62. PMID: 25525874 -
Nat Biotechnol
2018 Feb;36(2):179-189. PMID: 29251726 -
Immunity
Metabolic regulator LKB1 controls adipose tissue ILC2 PD-1 expression and mitochondrial homeostasis to prevent insulin resistance. [Abstract]2024 Jun 11;57(6):1289-1305.e9. PMID: 38772366 -
Nat Cancer
Targeting a lineage-specific PI3Kɣ-Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule. [Abstract]2024 Jul;5(7):1082-1101. PMID: 38816660
WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]
Growth inhibition curves (left panel), IC50 values, and AUCs (right panel) of OCI-AML2 cells treated with DMSO or 500nM ARM165 in combination with increasing doses (10-10000 nM）of either venetoclax, S63845, WEHI-539 and A-1331852. Error bars represent mean ± SD of three biological replicates composed of seven technical repeats after three days of seeding.
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Blood
Thrombopoietin/MPL signaling confers growth and survival capacity to CD41-positive cells in a mouse model of Evi1 leukemia. [Abstract]2014 Dec 4;124(24):3587-96. PMID: 25298035
WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Blood. 2014 Dec 4;124(24):3587-96. [Abstract]
CD41+ or CD41− cells are treated with DMSO as a vehicle control or a BCL-xL inhibitor (WEHI-539; 0.2, 0.4, and 0.8 μM) on OP9 stromal cells in the presence of THPO for 7 days. The number of viable cells is counted.
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2016 Mar 9:7:10916. PMID: 26956214 -
Nat Chem Biol
2022 Jun;18(6):615-624. PMID: 35332332 -
Cell Death Differ
Functional disparities among BCL-2 members in tonsillar and leukemic B-cell subsets assessed by BH3-mimetic profiling. [Abstract]2017 Jan;24(1):111-119. PMID: 27689871
WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2017 Jan;24(1):111-119. [Abstract]
BCL-XL-BIK complexes can be dissociated using the BCL-XL-inhibitor WEHI-539.
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Cell Death Differ
2014 Jul;21(7):1170-7. PMID: 24682005 -
Cell Death Dis
The identification of BCL-XL and MCL-1 as key anti-apoptotic proteins in medulloblastoma that mediate distinct roles in chemotherapy resistance. [Abstract]2023 Oct 28;14(10):705. PMID: 37898609 -
Pharmacol Res
Combination of palbociclib with navitoclax based-therapies enhances in vivo antitumoral activity in triple-negative breast cancer. [Abstract]2023 Jan:187:106628. PMID: 36566002 -
Cell Death Dis
Systems modeling accurately predicts responses to genotoxic agents and their synergism with BCL-2 inhibitors in triple negative breast cancer cells. [Abstract]2018 Jan 19;9(2):42. PMID: 29352235 -
Cell Death Dis
2017 Dec 13;8(12):3216. PMID: 29238043 -
Clin Cancer Res
2019 Dec 1;25(23):7139-7150. PMID: 31409615 -
Acta Pharmacol Sin
Chromosome instability functions as a potential therapeutic reference by enhancing chemosensitivity to BCL-XL inhibitors in colorectal carcinoma. [Abstract]2024 Nov;45(11):2420-2431. PMID: 39187678 -
Cell Rep
Drug-repurposing screen on patient-derived organoids identifies therapy-induced vulnerability in KRAS-mutant colon cancer. [Abstract]2023 Mar 30;42(4):112324. PMID: 37000626 -
Mol Cancer Ther
2025 Jul 10. PMID: 40635161 -
Breast Cancer Res Treat
Rationally derived drug combinations with the novel Mcl-1 inhibitor EU-5346 in breast cancer. [Abstract]2019 Feb;173(3):585-596. PMID: 30374681 -
J Ovarian Res
Antagonism of Bcl-XL is necessary for synergy between carboplatin and BH3 mimetics in ovarian cancer cells. [Abstract]2016 Apr 14:9:25. PMID: 27080533 -
Int J Cancer
Interleukin 8 mediates bcl-xL-induced enhancement of human melanoma cell dissemination and angiogenesis in a zebrafish xenograft model. [Abstract]2018 Feb 1;142(3):584-596. PMID: 28949016
WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2018 Feb 1;142(3):584-596. [Abstract]
Evaluation of PARP protein cleavage in Mneo and MXL90 cells after treatment for 24h with 20 μM NSC 119875, in presence of increasing doses of the specific Bcl-xL inhibitor WEHI-539.
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Oncol Rep
BH3 profiling discriminates the anti‑apoptotic status of 5‑fluorouracil‑resistant colon cancer cells. [Abstract]2019 Dec;42(6):2416-2425. PMID: 31638265 -
Am J Cancer Res
Glucocorticoid receptor antagonism overcomes resistance to BRAF inhibition in BRAFV600E-mutated metastatic melanoma. [Abstract]2019 Dec 1;9(12):2580-2598. PMID: 31911848 -
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Oncotarget
BCL2 and BCL(X)L selective inhibitors decrease mitochondrial ATP production in breast cancer cells and are synthetically lethal when combined with 2-deoxy-D-glucose. [Abstract]2018 May 25;9(40):26046-26063. PMID: 29899841
WEHI-539 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 May 25;9(40):26046-26063. [Abstract]
Representative images of Hoechst/PI merged channels for WEHI-539 treatment in MCF7-pSFFV cell line.
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvent & Solubility
DMSO : 16.67 mg/mL (26.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.03 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Ovcar-8, Ovcar-3, Ovcar-4 and Ovsaho cells are grown in the RPMI, Igrov-1, Cov-362 and Cov-318 cells are grown in DMEM and Fuov-1 cells are grown in DMEM/F-12 nutrient mixture. ABT-737, ABT-199 and WEHI-539 (Medchem Express, NJ, USA), are prepared as a 20 mM solution in DMSO. For cell growth assays, cells are plated in 96 wells plate (5,000 cells/well for all cell lines except Ovcar-8 which is plated at a density of 2,500 cells/well). The next day, cells are treated with drugs. After 72 h the culture medium is removed and the cells are fixed with 100 μL of cold 10 % Trichloroacetic acid (TCA), incubated on ice for 30 min and stained with 0.4 % sulforhodamine B (SRB). The data are analysed by using Graphpad Prism 4 software. Non-linear regression is used to fit a four parameters Hill equation. For drug combinations studies the cells are exposed simultaneously to a range of concentrations of NSC 241240 combined with fixed concentration of BH3 mimetics that is expected from the single agent studies to cause 5 % growth inhibition: ABT-737, 1 μM in Ovcar-8, Ovcar-3 and Igrov-1, 2 μM in Ovcar-4 and Ovsaho and 6 μM in Cov-362; ABT-199, 1 μM in Ovcar-4, 2 μM in Ovcar-3, Igrov-1, Cov-362 and Ovsaho and 3 μM in Ovcar-8; WEHI-539, 0.2 μM in Igrov-1, 0.3 μM in Ovcar-8, 1 μM in Ovcar-3 and Ovsaho, 3.1 μM in Cov-362 and 5 μM in Ovcar-4. Surviving cell number is assessed by SRB staining. A combination index (CI) is calculated[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Lessene G, et al. Structure-guided design of a selective BCL-X(L) inhibitor. Nat Chem Biol. 2013 Jun;9(6):390-7. [Content Brief]
[2]. Abed MN, et al. Antagonism of Bcl-XL is necessary for synergy between NSC 241240 and BH3 mimetics in ovarian cancer cells. J Ovarian Res. 2016 Apr 14;9:25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6124 mL | 8.0622 mL | 16.1244 mL | 40.3109 mL |
| 5 mM | 0.3225 mL | 1.6124 mL | 3.2249 mL | 8.0622 mL | |
| 10 mM | 0.1612 mL | 0.8062 mL | 1.6124 mL | 4.0311 mL | |
| 15 mM | 0.1075 mL | 0.5375 mL | 1.0750 mL | 2.6874 mL | |
| 20 mM | 0.0806 mL | 0.4031 mL | 0.8062 mL | 2.0155 mL | |
| 25 mM | 0.0645 mL | 0.3225 mL | 0.6450 mL | 1.6124 mL |
WEHI-539 hydrochloride Related Classifications
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