WNK463 Chemical Properties

Density 

1.43±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO : ≥ 30 mg/mL (64.73 mM)

pka

15.18±0.46(Predicted)

form 

Solid

color 

White to off-white

WNK463 Usage And Synthesis

Uses

WNK 463, is a pan-WNK kinase inhibitor, acting on WNK1, WNK2, WNK3, and WNK4 kinases. It has shown to affect blood pressure, heart rate, body fluid and electrolyte homeostasis in rodent models of hypertension.

Biochem/physiol Actions

WNK463 is a high-affinity, ATP-competitive inhibitor against with-No-Lysine (K) kinases (hWNK1/3/4 IC50 = 5/6/9 nM with MBP & 1 μM ATP, hWNK2 IC50 = 1 nM with MBP & 2 μM ATP, hWNK1 IC50 = 41 nM with OSR1 & 0.5 μM ATP; hWNK1/4 KD = 3.71/3.84 by SPR), exhibiting weak affinity against only two other human kinases among a panel of 442. WNK463 downregulates the overexpressed OSR1 phosphorylation level in HEK293 cells (IC50 = 106 nM; 1 hr) and displays in vivo efficacy in rodent hypertension models (1-10 mg/kg in rats p.o., 10 mg/kg in hWNK1 transgenic mice p.o.) with good orally availability (F = 100%/mice & 74%/rats post 1.5 mg/kg p.o.).

WNK463(2012607-27-9)Related Product Information

• Allosteric WNK Kinase Inhibitor ,