KN-93 Phosphate

Biological Activity

KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor, which has been implicated in the regulation of smooth muscle contractility. CaM kinase II activation was inhibited by KN-93 pretreatment (IC50 ~1 μM). KN-93 inhibited histamine-induced tonic Force maintenance, whereas early Force development and MLC20 phosphorylation responses during the entire time course were unaffected. Both Force development and maintenance in response to KCl were inhibited by KN-93. Rapid increases in KCl-induced MLC20 phosphorylation were also inhibited by KN-93, whereas steady-state MLC20 phosphorylation responses were unaffected. In contrast, phorbol 12,13-dibutyrate (PDBu) did not activate CaM kinase II and PDBu-stimulated Force development was unaffected by KN-93. Thus KN-93 appears to target a step(s) essential For Force maintenance in response to physiological stimuli, suggesting a role For CaM kinase II in regulating tonic contractile responses in arterial smooth muscle. Pharmacological activation of protein kinase C bypasses the KN-93 sensitive step.For the detailed information of KN-93, the solubility of KN-93 in water, the solubility of KN-93 in DMSO, the solubility of KN-93 in PBS buffer, the animal experiment (test) of KN-93, the cell expriment (test) of KN-93, the in vivo, in vitro and clinical trial test of KN-93, the EC50, IC50,and Affinity of KN-93, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.