WNK-IN-11

SKU: orb1301776

Description

WNK-IN-11 is a potent allosteric inhibitor of WNK1 kinase, exhibiting an IC50 of 4 nM. This small molecule is a valuable research tool for investigating WNK signaling pathways in hypertension and renal physiology through in vitro biochemical and cellular assays.

Research Area

Cell Biology, Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 2123489-30-3
• MW: 462.4
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₂₁Cl₂N₅OS
• SMILES: CNc1nc(cs1)-c1cc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c(Cl)cn1
• Target: Serine/threonin kinase,Serine Protease
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.65 mM);H2O:Insoluble;DMSO:150 mg/mL (324.39 mM)

Bioactivity

• Target IC50:
  WNK1:4 nM
• In Vitro:
  WNK-IN-11 (compound 11) demonstrates potent activity with an IC50 value of less than 2 μM in the OSR1 phosphorylation assay, exhibits reasonable water solubility, and shows relatively high microsomal clearance. It functions through ATP noncompetitive inhibition. When tested against a comprehensive panel of 440 human kinases at 10 μM, 2500-fold higher than the enzyme's IC50, WNK-IN-11 exhibits high selectivity, with significant off-target inhibition only against BTK and the feline encephalitis virus-related (FER) kinase, neither of which are involved in blood pressure regulation. This specificity highlights its potential as a targeted therapeutic agent, likely due to its predicted allosteric binding outside the conserved ATP-pocket region.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Allosteric WNK Kinase Inhibitor, Serine proteases, Serine kinase, Ser/Thr Protease, Serine endopeptidases, threoninkinase, Threonine proteases, threonin kinase, Serinekinase, WNKIN11, WNK-IN-11, WNK1, WNK IN 11

Compound Identifiers

PubChem CID

133080583