Cat. No.: HY-100626

WNK463

Name: WNK463
Brand: MedChemExpress
SKU: HY-100626
Price: 100.00 USD
Availability: InStock
Rating: 5 (21 reviews)

21 Cited Publications

고객리뷰

Based on 21 publication(s) in Google Scholar

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC_50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.75%
CAS No.: 2012607-27-9
화학식: C₂₁H₂₄F₃N₇O₂
분자량:463.46

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

WNK463 Chemical Structure

CAS No.: 2012607-27-9

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (21)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC_50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively^[1].

IC₅₀ & Target

WNK2

1 nM (IC₅₀)

WNK3

6 nM (IC₅₀)

WNK4

9 nM (IC₅₀)

WNK1

5 nM (IC₅₀)

All WNK Kinase Isoforms :

In Vitro

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.

Western Blot Analysis^[2]

Cell Line:

Human tissue-engineered corneas (hTECs)
Concentration:

50 nM, 1 μΜ, 10 μΜ
Incubation Time:

6 days
Result:

Reduced phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

In Vivo

WNK463 (1-10 mg/kg; oral administration; 4 hours; Spontaneously hypertensive Sprague Dawley rats) treatment produces dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. WNK463 produces significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates.
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.

Animal Model:

Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age) ^[1]
Dosage:

1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
Administration:

Oral administration; 4 hours
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

CAS No. 2012607-27-9
Appearance Solid
분자량 463.46
화학식 C₂₁H₂₄F₃N₇O₂
Color White to off-white
SMILES

FC(F)(F)C1=NN=C(O1)C2=CN=C(N3CCC(N4C=NC=C4C(NC(C)(C)C)=O)CC3)C=C2
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (21)

All Bio/Physico-chemical AssayCell Migration/Invasion AssayWBCell Imaging/StainingApoptosis Analysis

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Journal Impact Factor

Nat Metab

Slc12a8 is a nicotinamide mononucleotide transporter. [Abstract]

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.
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

Chloride sensing by WNK1 regulates NLRP3 inflammasome activation and pyroptosis. [Abstract]

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.
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.
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
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
Cancers (Basel)

WNK1 Kinase Stimulates Angiogenesis to Promote Tumor Growth and Metastasis. [Abstract]

2020 Mar 2;12(3):575. PMID: 32131390
J Innate Immun

Inhibition of WNK Kinases in NK Cells Disrupts Cellular Osmoregulation and Control of Tumor Metastasis. [Abstract]

2024;16(1):451-469. PMID: 39265537
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
SLAS Discov

Development of a BRET based chloride biosensor for high throughput screening of KCC2 modulators. [Abstract]

2025 Sep:35:100245. PMID: 40570963
SSRN

2026 Jul 22.
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
bioRxiv

2025 Sep 5.
Free University of Berlin

2024.
University of Berlin

2024 Mar 23.
bioRxiv

Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]

2023 Sep 12:2023.09.09.557001. PMID: 37745469
University College London

2021 Oct.

용액&용해도

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1577 mL

10.7884 mL

21.5768 mL

5 mM

0.4315 mL

2.1577 mL

4.3154 mL

10 mM

0.2158 mL

1.0788 mL

2.1577 mL

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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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WNK463

Publications Citing Use of MedChemExpress (MCE) WNK463

All WNK Kinase Isoforms