WNK463 | pan-WNK kinase inhibitor

CAS:
2012607-27-9
Catalog Number:
10-4109
Activity:
pan-WNK kinase inhibitor
Chemical Names:
N-tert-Butyl-3-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]pyridine-2-yl]piperidin-4-yl]imidazole-4-carboxamide
Molecular Weight:
463.47
Molecular Formula:
C21H24F3N7O2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$90.00
25 mg$325.00
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WNK463 (2012607-27-9) is a potent and selective pan-With-No-Lysine (WNK) kinase inhibitor (IC50’s: WNK1 = 5 nM, WNK2 = 1 nM, WNK3 = 6 nM, WNK4 = 9 nM), an important enzyme in blood pressure regulation and body fluid and electrolyte homeostasis.1 WNK kinases respond to hypertonicity by regulating SLC12 cation chloride transporters to rescue cell volume.2 WNK463 reduced migration of invasive types of breast cancer and attenuated tumor growth and metastatic burden in a mouse model.3 It induced a significant increase in NLRP3 inflammasome activation and pyroptosis specifically via WNK1 inhibition as well as increasing TNF production without inflammasome activation.4

Refences/Citations:

  1. Yamada et al. (2016), Small-molecule WNK inhibition regulates cardiovascular and renal function; Nat. Chem. Biol. 12 896
  2. Boyd-Shiwarski et al. (2022), WNK kinases sense molecular crowding and rescue cell volume via phase separation; Cell 185 4488
  3. Jaykumar et al. (2021), WNK1 Enhances Migration and Invasion in Breast Cancer Models; Mol. Cancer Ther. 20 1800
  4. Mayes-Hopfinger et al. (2021), Chloride sensing by WNK1 regulates NLRP3 inflammasome activation and pyroptosis; Nat. Commun. 12 4546
CAS:
2012607-27-9
Catalog Number:
10-4109
Activity:
pan-WNK kinase inhibitor
Chemical Names:
N-tert-Butyl-3-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]pyridine-2-yl]piperidin-4-yl]imidazole-4-carboxamide
Molecular Weight:
463.47
Molecular Formula:
C21H24F3N7O2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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