1. Membrane Transporter/Ion Channel
  2. WNK Kinase
  3. WNK463

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.

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No. CAS : 2012607-27-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO En stock
Solid
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Revisión del cliente

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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.

    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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    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    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[1].

    IC50 & Target

    WNK2

    1 nM (IC50)

    WNK3

    6 nM (IC50)

    WNK4

    9 nM (IC50)

    WNK1

    5 nM (IC50)

    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.
    Peso molecular

    463.46

    Fòrmula

    C21H24F3N7O2

    No. CAS
    Appearance

    Solid

    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

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvente y solubilidad
    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1577 mL 10.7884 mL 21.5768 mL
    5 mM 0.4315 mL 2.1577 mL 4.3154 mL
    View the 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Pureza y Documentación

    Purity: 99.75%

    Referencias

    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
    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    Nombre del producto:
    WNK463
    Cat. No.:
    HY-100626
    Cantidad:
    MCE Japan Authorized Agent: