WNK-IN-11是(WNK)激酶的变构抑制剂，其对WNK1的IC50值为4nM。
CAS：2123489-30-3
分子式：C21H21Cl2N5OS
分子量：462.4
纯度：98%
存储：Store at -20°C

Background:

WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.

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].

[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.