名称 | KN-62 |
描述 | KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM. |
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) |
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. |
体外活性 | KN-62 administration in adult rats reduces the expression levels of brain-derived neurotrophic factor (BDNF) mRNA induced by epilepsy in the brain. |
体内活性 | KN-62 inhibits the proliferation of K562 cells and blocks cell cycle progression. When administered at 10 μM to rat pancreatic islet cells, KN-62 inhibits insulin secretion stimulated by carbachol and potassium. Furthermore, KN-62 suppresses the phosphorylation of Ca2+/CaM kinase induced by A23187 in PC12 D cells. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 72.2 mg/mL (100 mM)
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关键字 | noncompetitive antagonism | inhibit | KN62 | P2XRs | KN-62 | Calmodulin-dependent protein kinases | HEK293 cells | KN 62 | P2X Receptor | Calmodulin-dependent kinases | CaMK | Inhibitor | autophosphorylation |
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