WNK463
Based on 20 publication(s) in Google Scholar
WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 2012607-27-9
- Formula: C21H24F3N7O2
- Molecular Weight:463.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) WNK463
More- Nat Metab. 2019 Jan;1(1):47-57. [Abstract]
- Nat Commun. 2025 May 27;16(1):4920. [Abstract]
- Nat Commun. 2025 Feb 21;16(1):1857. [Abstract]
- Nat Commun. 2021 Jul 27;12(1):4546. [Abstract]
- Cell Rep. 2024 May 8;43(5):114211. [Abstract]
- Sci Signal. 2024 Aug 27;17(851):eade1119. [Abstract]
- Int J Mol Sci. 2022 Oct 11;23(20):12100. [Abstract]
- RMD Open. 2025 Jul 1;11(3):e005707. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- Cancers. 2020 Mar 2;12(3):575. [Abstract]
- Sci Rep. 2026 Feb 5. [Abstract]
- Mol Carcinog. 2024 Jan;63(1):173-189. [Abstract]
- J Innate Immun. 2024 Sep 12:1-24. [Abstract]
- SLAS Discov. 2025 Jun 24:100245. [Abstract]
- bioRxiv. 2026 Jun 12:2026.06.10.731153. [Abstract]
- bioRxiv. 2025 Sep 5.
- Free University of Berlin. 2024.
- University of Berlin. 2024 Mar 23.
- bioRxiv. 2023 Sep 12:2023.09.09.557001. [Abstract]
- University College London. 2021 Oct.
Customer Validation & Images
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WB
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Apoptosis Analysis
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Cell Migration/Invasion Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
Biological Activity
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WNK2 1 nM (IC50) |
WNK3 6 nM (IC50) |
WNK4 9 nM (IC50) |
WNK1 5 nM (IC50) |
WNK463 (50 nM, 1 μΜ, 10 μΜ; 6 days; Human tissue-engineered corneas (hTECs)) treatment reduces phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human tissue-engineered corneas (hTECs)
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Concentration:50 nM, 1 μΜ, 10 μΜ
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Incubation Time:6 days
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Result:Reduced phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.
WNK463 is orally bioavailable in Sprague Dawley rats with a half-life of 2.1 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age) [1]
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Dosage:1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
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Administration:Oral administration; 4 hours
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Result:Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.
Chemical Information
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CAS No. 2012607-27-9
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Appearance Solid
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Molecular Weight 463.46
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Formula C21H24F3N7O2
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Color White to off-white
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SMILES
FC(F)(F)C1=NN=C(O1)C2=CN=C(N3CCC(N4C=NC=C4C(NC(C)(C)C)=O)CC3)C=C2
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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 (20)
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Journal Impact Factor
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Most Recent
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Nat Metab
2019 Jan;1(1):47-57. PMID: 31131364 -
Nat Commun
WNK1 signalling regulates amino acid transport and mTORC1 activity to sustain acute myeloid leukaemia growth. [Abstract]2025 May 27;16(1):4920. PMID: 40425534
WNK463 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 27;16(1):4920. [Abstract]
WNK463 (0.01, 0.1, 1, 10, 100 μM) produced a dose-dependent inhibition of WNK1 activity as measured by the reduction of phosphorylation of the WNK kinase substrates OXSR1 and STK39.
WNK463 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 27;16(1):4920. [Abstract]
WNK463 (1, 3, 10 μM) treatment significantly induced apoptosis in primary AML samples.
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Nat Commun
WNK1-dependent water influx is required for CD4+ T cell activation and T cell-dependent antibody responses. [Abstract]2025 Feb 21;16(1):1857. PMID: 39984435 -
Nat Commun
2021 Jul 27;12(1):4546. PMID: 34315884
WNK463 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jul 27;12(1):4546. [Abstract]
An increase in lactate dehydrogenase (LDH) release in cells treated with ATP, Nigericin, or MSU in the presence of WNK463 (1 μM) compared with controls.
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Cell Rep
Identification of WNK1 as a therapeutic target to suppress IgH/MYC expression in multiple myeloma. [Abstract]2024 May 8;43(5):114211. PMID: 38722741 -
Sci Signal
Chemokine-mediated F-actin dynamics, polarity, and migration in B lymphocytes depend on WNK1 signaling. [Abstract]2024 Aug 27;17(851):eade1119. PMID: 39190707
WNK463 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2024 Aug 27;17(851):eade1119. [Abstract]
2PK-3 cells pretreated with DMSO, or the indicated concentrations of WNK463 (0.3, 1, 3, 5 μM) or WNK-IN-11 were subjected to a transwell migration assay with CXCL13 (1 μg/mL).
WNK463 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2024 Aug 27;17(851):eade1119. [Abstract]
LifeAct B cells were treated with WNK463 (5 μM) or not and subjected to under agarose migration assay on glass-bottom culture dishes coated with ICAM-1/Fc, CXCL12, and CXCL13.
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Int J Mol Sci
WNK1-OSR1 Signaling Regulates Angiogenesis-Mediated Metastasis towards Developing a Combinatorial Anti-Cancer Strategy. [Abstract]2022 Oct 11;23(20):12100. PMID: 36292952 -
RMD Open
WNK2 variants associated with familial osteoarthritis alter the chondrocyte response to hyperosmotic stress. [Abstract]2025 Jul 1;11(3):e005707. PMID: 40592720 -
Toxicology
Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]2024 May 15:505:153830. PMID: 38754619 -
Cancers
2020 Mar 2;12(3):575. PMID: 32131390 -
Sci Rep
Knock-down of the long isoform of the WNK1 kinase mitigates the anti-glomerular basement membrane glomerulonephritis in mice. [Abstract]2026 Feb 5. PMID: 41644982 -
Mol Carcinog
Focal adhesion kinase confers lenvatinib resistance in hepatocellular carcinoma via the regulation of lysine-deficient kinase 1. [Abstract]2024 Jan;63(1):173-189. PMID: 37787401 -
J Innate Immun
Inhibition of WNK Kinases in NK Cells Disrupts Cellular Osmoregulation and Control of Tumor Metastasis. [Abstract]2024 Sep 12:1-24. PMID: 39265537 -
SLAS Discov
Development of a BRET based chloride biosensor for high throughput screening of KCC2 modulators. [Abstract]2025 Jun 24:100245. PMID: 40570963 -
bioRxiv
WNK-SPAK/OSR1 signaling pathway facilitates ictal activity via reduced neuronal chloride extrusion rate. [Abstract]2026 Jun 12:2026.06.10.731153. PMID: 42327210 -
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bioRxiv
Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]2023 Sep 12:2023.09.09.557001. PMID: 37745469 -
Solvent & Solubility
DMSO : ≥ 30 mg/mL (64.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
Purity & Documentation
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Data Sheet (276 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]. Yamada K et al. Small-molecule WNK inhibition regulates cardiovascular and renal function. Nat Chem Biol. 2016 Nov;12(11):896-898. [Content Brief]
[2]. Desjardins P, et al. Contribution of the WNK1 kinase to corneal wound healing using the tissue-engineered human cornea as an in vitro model. J Tissue Eng Regen Med. 2019 Sep;13(9):1595-1608. [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. 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 |
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| DMSO | 1 mM | 2.1577 mL | 10.7884 mL | 21.5768 mL | 53.9421 mL |
| 5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL | 10.7884 mL | |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1577 mL | 5.3942 mL | |
| 15 mM | 0.1438 mL | 0.7192 mL | 1.4385 mL | 3.5961 mL | |
| 20 mM | 0.1079 mL | 0.5394 mL | 1.0788 mL | 2.6971 mL | |
| 25 mM | 0.0863 mL | 0.4315 mL | 0.8631 mL | 2.1577 mL | |
| 30 mM | 0.0719 mL | 0.3596 mL | 0.7192 mL | 1.7981 mL | |
| 40 mM | 0.0539 mL | 0.2697 mL | 0.5394 mL | 1.3486 mL | |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 1.0788 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3596 mL | 0.8990 mL |
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