1188890-41-6

KN-93 (phosphate) is a potent and selective inhibitor of Ca²⁺/calmodulin-dependent kinase II (CaMKII) (K_i = 370 nM), inhibiting both the α- and β-subunits of CaMKII. It does not have significant effects on cAMP-dependent protein kinase, Ca²⁺/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca²⁺ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC₅₀ = 300 nM). KN-93 can block voltage-gated potassium (K_v) channels when applied extracellularly, independent of its CaMKII action. More recently, KN-93 has been used to implicate roles for CaMKII in Ca²⁺-induced Ca²⁺ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca²⁺-dependent activation of HIF-1α in colon cancer cells.

Selective inhibitor of rat brain Ca2+/calmodulin-dependent protein kinase II. Inhibits glucose-induced and forskolin-stimulated insulin release from isolated pancreatic islets of Langerhans. Has no significant effect on protein kinase A (PKA) activity. Induces G1 cell cycle arrest and apoptosis in NIH 3T3 cells.

CaMK IIα

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