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WNK-IN-11 (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 (Allosteric WNK Kinase Inhibitor) 是(WNK)激酶的变构抑制剂,能够抑制 WNK1 (IC50:4 nM) 。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 762 | 现货 | |
5 mg | ¥ 1,830 | 现货 | |
10 mg | ¥ 3,130 | 现货 | |
25 mg | ¥ 5,170 | 现货 | |
50 mg | ¥ 7,320 | 现货 | |
100 mg | ¥ 9,870 | 现货 | |
500 mg | ¥ 19,700 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,930 | 现货 |
产品描述 | WNK-IN-11 (Allosteric WNK Kinase Inhibitor) is an allosteric With-No-Lysine (WNK) kinase inhibitor,WNK1(IC50 : 4 nM) |
靶点活性 | WNK1:4 nM |
体外活性 | 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. |
别名 | Allosteric WNK Kinase Inhibitor |
分子量 | 462.4 |
分子式 | C21H21Cl2N5OS |
CAS No. | 2123489-30-3 |
Smiles | CNc1nc(cs1)-c1cc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c(Cl)cn1 |
密度 | 1.407 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: Insoluble DMSO: 150 mg/mL (324.39 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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