KN-93
KN-93 is an inhibitor of calmodulin-dependent kinase II (CaMKII); it may also inhibit L-type Ca2+ channels. KN-93 exhibits anticancer, anti-arrhythmic, cardiomodulatory, antinociceptive, and immunomodulatory activities. In vitro, KN-93 decreases VEGF expression. When combined with VEGF inhibitors, this compound decreases tumor growth in animal models of cancer. In other animal models, KN-93 prevents the development of arrhythmia and increases levels of Treg cells. KN-93 also increases withdrawal latency in animal models of thermal and mechanical pain.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18936696
| Cas No. |
1188890-41-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C26H29ClN2O4S・H3O4P |
| Formula Wt. |
599.03 |
| IUPAC Name |
N-[2-({[(2E)-3-(4-Chlorophenyl)-2-propen-1-yl](methyl)amino}methyl)phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate (1:1) |
| Synonym |
2-[N-(2-Hydroxyethyl)-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine |
| Solubility |
Soluble in water |
| Appearance |
White to off-white solid. |
Takeuchi M, Yamamoto T. Apoptosis induced by NAD depletion is inhibited by KN-93 in a CaMKII-independent manner. Exp Cell Res. 2015 Jul 1;335(1):62-7. PMID: 26024774.
Tzimas C, Terrovitis J, Lehnart SE, et al. Calcium/calmodulin-dependent protein kinase II (CaMKII) inhibition ameliorates arrhythmias elicited by junctin ablation under stress conditions. Heart Rhythm. 2015 Jul;12(7):1599-610. PMID: 25814413.
Daft PG, Yang Y, Napierala D, et al. The growth and aggressive behavior of human osteosarcoma is regulated by a CaMKII-controlled autocrine VEGF signaling mechanism. PLoS One. 2015 Apr 10;10(4):e0121568. PMID: 25860662.
Bian H, Yu LC. Intra-nucleus accumbens administration of the calcium/calmodulin-dependent protein kinase II inhibitor KN93 induced antinociception in rats with mononeuropathy. Neurosci Lett. 2014 Nov 7;583:6-10. PMID: 25218714.
Koga T, Mizui M, Yoshida N, et al. KN-93, an inhibitor of calcium/calmodulin-dependent protein kinase IV, promotes generation and function of Foxp3⁺ regulatory T cells in MRL/lpr mice. Autoimmunity. 2014 Nov;47(7):445-50. PMID: 24829059.
