Home Apoptosis Serine/threonin kinase inhibitor WNK463 For research use only.

WNK463

WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4) with IC50 of 5nM, 1nM, 6nM, and 9nM.

WNK463 Chemical Structure

WNK463 Chemical Structure

CAS: 2012607-27-9

Selleck's WNK463 has been cited by 10 publications

Purity & Quality Control

Batch: Purity: 99.76%
99.76

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Choose Selective Serine/threonin kinase Inhibitors

Biological Activity

Description WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4) with IC50 of 5nM, 1nM, 6nM, and 9nM.
Targets
WNK2 [1] WNK1 [1] WNK3 [1] WNK4 [1]
1nM 5nM 6nM 9nM
In vitro
In vitro

WNK463 potently inhibited the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). WNK463 also inhibited WNK1-catalyzed phosphorylation of the native WNK substrate, oxidative stress response 1 (OSR1) in a biochemical assay and in human embryonic kidney 293 (HEK293) cells that express exogenous OSR1 and that are activated by sorbitol-mediated osmotic stress[1].
Cell Research Cell lines HUVECs
Concentrations 1 µM
Incubation Time 6 h
Method

Cells were treated with indicated concentration of drug for 6 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pSPAK/pOSR1 31207112
In Vivo
In vivo

In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electrolyte homeostasis. WNK463 is orally bioavailable in C57BL/6 mice (100%) and Sprague Dawley rats (74%), with a half-life of 3.6 and 2.1 h, respectively. In spontaneously hypertensive rats (SHRs), WNK463 administered orally (p.o.) at 1, 3, or 10 mg per kg body weight (mg/kg) p.o. achieved maximum plasma concentration (Cmax) values of 88, 441, and 1,170 nM, respectively. These exposures produced dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. Moreover, WNK463 produced significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates. Orally administered WNK463 also significantly decreased blood pressure in these hypertensive mice. WNK463 elicited in vivo cardiovascular and renal effects through WNK kinase inhibition[1].
Animal Research Animal Models Male Sprague Dawley rats or male C57BL/6 mice
Dosages 1 mg/kg(i.v.) or 3 mg/kg (oral)
Administration i.v. or oral administration

Chemical Information & Solubility

Molecular Weight 463.46 Formula

C21H24F3N7O2
CAS No. 2012607-27-9 SDF Download WNK463 SDF
Smiles CC(C)(C)NC(=O)C1=CN=CN1C2CCN(CC2)C3=NC=C(C=C3)C4=NN=C(O4)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (198.5 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 92 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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