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KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。


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KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 285 | In stock | |
| 2 mg | ¥ 397 | In stock | |
| 5 mg | ¥ 663 | In stock | |
| 10 mg | ¥ 1,080 | In stock | |
| 25 mg | ¥ 2,290 | In stock | |
| 50 mg | ¥ 3,430 | In stock | |
| 100 mg | ¥ 4,890 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 795 | In stock |
KN-62 相关产品
| 产品描述 | KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM. |
| 靶点活性 | CaMK II:0.9 μM(Ki), CaMK V:0.8 μM(Ki) |
| 体外活性 | KN-62作用于成年大鼠,降低其脑中癫痫诱导的脑源性神经生长因子mRNA的表达水平. |
| 体内活性 | KN-62抑制K562细胞的增殖,并阻断细胞周期进程。10 μM KN-62作用于大鼠胰岛细胞,抑制卡巴胆碱和钾刺激的胰岛素分泌。KN-62抑制PC12 D细胞中A23187诱导的Ca2+/CaM激酶磷酸化作用。 |
| 激酶实验 | Kinase assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid. |
| 细胞实验 | For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted. (Only for Reference) |
| 分子量 | 721.84 |
| 分子式 | C38H35N5O6S2 |
| CAS No. | 127191-97-3 |
| Smiles | O=C([C@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)NCS(=O)(=O)c1cccc2cnccc12)N1CCN(CC1)c1ccccc1 |
| 密度 | 1.388 g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 72.2 mg/mL (100.02 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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