KN-93 (hydrochloride)

1956426-56-4

C26H30Cl2N2O4S

H2O : 0.45 mg/mL (0.84 mM; Need ultrasonic and warming); DMSO : >= 31 mg/mL (57.67 mM)

Neuronal Signaling

KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a K_i of 370 nM. IC50 & Target: Ki: 370 nM (CaMK-II) 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 uM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca²⁺-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93^[3].