WNK inhibitor 11

SKU: orb1225677

Description

WNK inhibitor 11 is a potent, selectiive and orally active inhibitor of WNK1 kinase with IC50 of 6 nM, 1,000-fold selectivity over WNK4 and 57-fold selectivity over WNK2; shows excellent selectivity with only a few significant off-target kinase inhibitions, most notably BTK and FER kinase; reduces blood pressure in mice overexpressing human WNK1, and induced diuresis, natriuresis and kaliuresis in spontaneously hypertensive rats.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2123489-30-3
• MW: 462.393
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₁Cl₂N₅OS
• SMILES: O=C(C1=CC(C2=CSC(NC)=N2)=NC=C1Cl)N3CCN(CC4=CC=C(Cl)C=C4)CC3
• Target: WNK Kinase
• Solubility: DMSO : 150 mg/mL 324.39 mM;H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  WNK-IN-11 (compound 11) shows IC50<2 μM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility, albeit with still rather high microsomal clearance. WNK-IN-11 shows ATP noncompetitive inhibition. When tested against a panel of 440 human kinases at 10 μM concentration, 2500-fold above enzyme IC50 value, WNK-IN-11 shows excellent selectivity with only a few significant off-target kinase inhibitions, most notably BTK and feline encephalitis virus-related (FER) kinase, neither of which are implicated for blood pressure regulation. This excellent selectivity profile is consistent with the predicted allosteric binding mode outside the highly conserved ATP-pocket.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WNK-IN-11 | WNK IN 11 | WNKIN11 | WNK inhibitor 11 | WNK inhibitor-11 |

Quick Database Links

Gene Symbol

WNK Kinase