WNK-IN-11
Names
[ CAS No. ]:
2123489-30-3
[ Name ]:
WNK-IN-11
Biological Activity
[Description]:
WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
[Related Catalog]:
[Target]
IC50: 4 nM (WNK1)[1].
[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[1].
[References]
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Chemical & Physical Properties
[ Molecular Formula ]:
C21H21Cl2N5OS
[ Molecular Weight ]:
462.4
[ Storage condition ]:
-20℃