KN-93 Phosphate

KN-93 PhosphateCAS号: 1913269-12-1分子式: C26H32ClN2O8PS分子量: 599.03描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II with K i of 370 nM. KN-93 phosphate inhibits serum-induced fibroblast cell growth in a comparable dose-dependent fashion to its inhibition of CaMK-II activity.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
H2O:84 mg/mL (140.2 mM),DMSO:93 mg/mL (155.3 mM)
生物活性
靶点
CaMKII:0.37 μM(Ki)
In vitro(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 [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 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca 2+ -independent CaM kinase activity is increased during early afterdepolarizations. The increase in CaM kinase activity is prevented by pretreatment with KN-93 [3].