2123489-30-3

2123489-30-3 structure

Name: WNK-IN-11
Chemical Name: WNK-IN-11
CAS Number: 2123489-30-3
Molecular Formula: C₂₁H₂₁Cl₂N₅OS
Molecular Weight: 462.4
Catalog: Research Areas Others
Create Date: 2019-01-20 09:38:19
Modify Date: 2024-01-10 17:44:55
WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.

Name	WNK-IN-11

Description	WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Others
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	[1]. Yamada K, et al. Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models. J Med Chem. 2017 Aug 24;60(16):7099-7107.