WEHI-539
Based on 30 publication(s) in Google Scholar
WEHI-539 is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
For research use only. We do not sell to patients.
- CAS No.: 1431866-33-9
- Formula: C31H29N5O3S2
- Molecular Weight:583.72
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) WEHI-539
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(1):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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H146 | EC50 |
550 nM
Compound: 3, WEHI-539
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Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum
Cytotoxicity against BCL-XL-dependent human NCI-H146 cells in presence of 10% human serum
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[PMID: 25313317] |
WEHI-539 is a selective inhibitor of Bcl-XL. WEHI-539 augments Carboplatin 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. 1431866-33-9
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Appearance Solid
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Molecular Weight 583.72
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Formula C31H29N5O3S2
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Color Light yellow to 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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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 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 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(1):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 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 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
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 carboplatin 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 (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 carboplatin and BH3 mimetics in ovarian cancer cells. J Ovarian Res. 2016 Apr 14;9:25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WEHI-539 Related Classifications
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