|Description||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.|
|Synonyms||KN 93; KN93|
Syntide 2, a synthetic peptide, is recognized as a substrate by Ca2+/calmodulin-dependent protein kinase II (CaMKII) (Ki= 12 μM) and protein kinase C (Km = 11 µ...
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.
KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopy...
Arcyriaflavin A is a potent dual target agent of calcium/calmodulin-dependent protein kinase II (CaMKII) and cyclin-dependent kinase 4 (CDK4). Its IC50 values a...
KN 93 is an inhibitor of multifunctional Calmodulin-dependent protein kinase (CaMKII; Ki value 0.37 μM for inhibition of CaMKII phosphorylating activity). KN93 ...
KN-92 is an inactive analog of the CaM kinase II inhibitor KN 93.
MLCK inhibitor peptide 18
A myosin light chain kinase (MLCK) inhibitor (IC50= 50 nM), and inhibits CaM kinase IIonly at 4000-fold higher concentrations.
KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII). At concentrations up to 25 μM, KN-92 is ...