A WNK1-4 inhibitor
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WNK463

Item No. 37673

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-1H-imidazole-5-carboxamide
CAS Number
2012607-27-9
Molecular Formula
C21H24F3N7O2
Formula Weight
463.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Soluble
SMILES
FC(F)(F)C(O1)=NN=C1C2=CC=C(N=C2)N3CCC(N4C(C(NC(C)(C)C)=O)=CN=C4)CC3
InChi Code
InChI=1S/C21H24F3N7O2/c1-20(2,3)27-17(32)15-11-25-12-31(15)14-6-8-30(9-7-14)16-5-4-13(10-26-16)18-28-29-19(33-18)21(22,23)24/h4-5,10-12,14H,6-9H2,1-3H3,(H,27,32)
InChi Key
HWSHOMMVLGBIDN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $87

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    10 mg

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    25 mg

    $348

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    50 mg

    $653

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    Product Description

    WNK463 is an inhibitor of WNK lysine-deficient protein kinase 1 (WNK1), WNK2, WNK3, and WNK4 (IC50s = 5, 1, 6, and 9 nM, respectively).1 It is selective for WNK1-4 over a panel of 442 kinases at 10 µM. In vivo, WNK463 (1, 3, and 10 mg/kg) decreases blood pressure, as well as increases urine output and urinary sodium and potassium excretion rates in spontaneously hypertensive rats (SHRs). It also decreases tumor growth, induces intratumoral apoptosis, and increases intratumoral levels of CD4+ and CD8+ T cells in an MC-38 mouse syngeneic colon cancer model when administered at doses of 5 and 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yamada, K., Park, H.-M., Rigel, D.F., et al. Small-molecule WNK inhibition regulates cardiovascular and renal function. Nat. Chem. Biol. 129(11), 896-898 (2016).

    2. Yoon, H.J., Kim, G.-C., Oh, S., et al. WNK3 inhibition elicits antitumor immunity by suppressing PD-L1 expression on tumor cells and activating T-cell function. Exp. Mol. Med. 54(11), 1913-1926 (2022).