KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
体外研究
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. 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. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells.
体内研究
KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina.
分子式
C26H29ClN2O4S
分子量
501.04
CAS号
139298-40-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : ≥ 50 mg/mL (99.79 mM)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)