WNK inhibitor 11

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WNK抑制剂11是一种有效的、选择性的、口服活性的WNK1激酶抑制剂，IC50为6 nM，选择性是WNK4的1,000倍，是WNK2的57倍。

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.

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

Autophagy

WNK Kinase

WNK Kinase

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2123489-30-3

462.393

C21H21Cl2N5OS

>98% (HPLC)

DMSO : 150 mg/mL 324.39 mM;H2O : < 0.1 mg/mL

O=C(C1=CC(C2=CSC(NC)=N2)=NC=C1Cl)N3CCN(CC4=CC=C(Cl)C=C4)CC3

(5-chloro-2-(2-(methylamino)thiazol-4-yl)pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone

(-20℃)

With Ice Pack

≥ 2 years