ALLOSTERIC WNK KINASE INHIBITOR
中文名称 | ALLOSTERIC WNK KINASE INHIBITOR |
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中文同义词 | 5-氯-2-[2-(甲氨基)-4-噻唑基]-4-吡啶基][4-[(4-氯苯基)甲基]-1-哌嗪基]-甲酮;化合物WNK-IN-11;优选][PERFEMIKER]WNK-IN-11 |
英文名称 | Allosteric WNK Kinase Inhibitor , |
英文同义词 | ALLOSTERIC WNK KINASE INHIBITOR;Allosteric WNK Kinase Inhibitor ,;WNK-IN-11;WNK-IN-11; WNK IN 11; WNKIN11; WNK INHIBITOR 11; WNK INHIBITOR-11;2123489-30-3;(5-Chloro-2-(2-(methylamino)thiazol-4-yl)pyridin-4-yl)(4-(4-chlorobenzyl)piperazin-1-yl)methanone;Methanone, [5-chloro-2-[2-(methylamino)-4-thiazolyl]-4-pyridinyl][4-[(4-chlorophenyl)methyl]-1-piperazinyl]-;Threonine proteases,inhibit,WNKIN11,Serine proteases,Serine endopeptidases,Inhibitor,Ser/Thr Protease,WNK IN 11 |
CAS号 | 2123489-30-3 |
分子式 | C21H21Cl2N5OS |
分子量 | 462.4 |
EINECS号 | |
相关类别 | |
Mol文件 | 2123489-30-3.mol |
结构式 |
ALLOSTERIC WNK KINASE INHIBITOR 性质
沸点 | 641.1±65.0 °C(Predicted) |
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密度 | 1.407±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMF:30mg/mL; DMF:PBS (pH 7.2) (1:10):0.1 mg/mL; DMSO:25mg/mL;乙醇:3mg/mL |
形态 | 结晶固体 |
酸度系数(pKa) | 5.52±0.10(Predicted) |
Target | Value |
WNK1
(Cell-free assay) | 4 nM |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-112094 | WNK-IN-11 | 1 mg | 920元 | |
2024/01/25 | HY-112094 | ALLOSTERIC WNK KINASE INHIBITOR WNK-IN-11 | 2123489-30-3 | 5mg | 2300元 |