ALLOSTERIC WNK KINASE INHIBITOR

ALLOSTERIC WNK KINASE INHIBITOR化学性质

沸点 :641.1±65.0 °C(Predicted)
密度 :1.407±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:10): 0.1 mg/ml; DMSO: 25 mg/ml; Ethanol: 3 mg/ml
形态 :A crystalline solid
酸度系数(pKa) :5.52±0.10(Predicted)
颜色 :White to off-white

ALLOSTERIC WNK KINASE INHIBITOR性质、用途与生产工艺

生物活性 WNK-IN-11 是一种有效的、具有选择性的 With-No-Lysine (WNK) 的口服活性变构抑制剂，对WNK1酶的IC50为4 nM。
靶点
Target Value
WNK1
(Cell-free assay) 4 nM
体外研究

WNK-IN-11 (compound 11) shows IC ₅₀ <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 IC ₅₀ 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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ALLOSTERIC WNK KINASE INHIBITOR生产厂家

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Target	Value
WNK1 (Cell-free assay)	4 nM