Allosteric WNK Kinase Inhibitor 是(WNK)激酶的变构抑制剂，能够抑制 WNK1 (IC50:4 nM) 。

WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor,WNK1(IC50 : 4 nM)

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.

2123489-30-3

C21H21Cl2N5OS

462.39

Allosteric WNK Kinase Inhibitor

DMSO:150 mg/mL (324.39 mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years