KN93 hydrochloride Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF:10.0(Max Conc. mg/mL);18.6(Max Conc. mM)
DMSO:20.5(Max Conc. mg/mL);38.14(Max Conc. mM)
Water:0.45(Max Conc. mg/mL);0.84(Max Conc. mM)

form 

A crystalline solid

color 

White to off-white

KN93 hydrochloride Usage And Synthesis

Uses

KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.

Biological Activity

KN93 hydrochloride is a cell-permeable, reversible and competitive inhibitor of calmodulin-dependent kinase type II (CaMKII) with Ki of 370 nM.

in vitro

After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN93 release, a peak of cells had progressed into S and G2-M. KN93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts.

target

IC 50

CaMK II

References

[1] Tombes RM, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK-II (the multifunctional Ca2+/CaM kinase). Cell Growth Differ. 1995 Sep;6(9):1063-70. PMID:8519682
[2] Li J, et al. Curcumin Attenuates Retinal Vascular Leakage by Inhibiting Calcium/Calmodulin-Dependent Protein Kinase II Activity in Streptozotocin-Induced Diabetes. Cell Physiol Biochem. 2016;39(3):1196-208. DOI:10.1159/000447826
[3] Mamiya N, et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitorKN-93. Biochem Biophys Res Commun. 1993 Sep 15;195(2):608-15. DOI:10.1006/bbrc.1993.2089
[4] Anderson ME, et al. KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006. PMID:9864285