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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-15531
VenetoclaxBCL-2 Inhibitor -
HY-10087
NavitoclaxBcl-2 Inhibitor -
HY-50907
ABT-737Bcl-2 Family Inhibitor/BH3 Mimetic -
HY-19741
A-1331852Bcl-xL Inhibitor -
HY-18628
UMI-77Bcl-2 Family Inhibitor -
HY-10969
Obatoclax MesylateBcl-2 Family Inhibitor -
HY-15531R
Venetoclax (Standard)BCL-2 Inhibitor -
HY-100741
S63845MCL1 Inhibitor -
HY-10087R
Navitoclax (Standard)Reference Standard -
HY-12011
HA14-1Bcl-2 Family Inhibitor -
HY-103269
BAI1BAX Inhibitor -
HY-12468
A-1210477Mcl-1 Inhibitor
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]
- 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]
- Breast Cancer Res Treat. 2019 Feb;173(3):585-596. [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
Description
IC50 & Target
[1]|
Bcl-xL 1.1 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 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] |
In Vitro
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. Further protocols information, click here.
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 -
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 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 -
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 -
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
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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
HY-15607 Related Classifications
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