| Description | KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II with K i of 370 nM. KN-93 phosphate inhibits serum-induced fibroblast cell growth in a comparable dose-dependent fashion to its inhibition of CaMK-II activity. |
| In vitro | After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts [1]. KN-93 inhibits the H +, K + -ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space [2]. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca 2+ -independent CaM kinase activity is increased during early afterdepolarizations. The increase in CaM kinase activity is prevented by pretreatment with KN-93 [3]. |
| Cell experiments | NIH 3T3 fibroblasts are cultured on polystyrene dishes in DMEM and fetal bovine serum, supplemented with penicillin/streptomycmn in a 5% CO2 humidified chamber at 37 癈. Cell growth is measured by using the MTT dye reduction method. (Only for Reference) |
| Target activity | CaMK II:0.37 μM(Ki) |
| molecular weight | 599.03 |
| Molecular formula | C26H32ClN2O8PS |
| CAS | 1913269-12-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 93 mg/mL (155.3 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 84 mg/mL (140.2 mM) |
| References | 1. Sumi M, et al. Biochem Biophys Res Commun. 1991, 181(3), 968-975. 2. Tombes RM, et al. Cell Growth Differ. 1995, 6(9), 1063-1070. 3. Rokhlin OW, et al. Cancer Biol Ther. 2010, 9(3), 224-235. 4. Yang X, et al. Neuropsychiatr Dis Treat. 2013, 9, 1213-1220. 5. Koga T, et al. Autoimmunity. 2014, 15, 1-6. |