KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM..
KN-62 exhibits strong antagonism against ATP-induced Ba2+ influx in fura-2-loaded human lymphocytes, with an IC50 of 12.7 nM and complete inhibition of the flux at a concentration of 500 nM[1]. KN-62 does not hinder the activity of autophosphorylated Ca2+/CaM kinase II. It dose-dependently inhibits the Ca2+/calmodulin-dependent autophosphorylation of both alpha (50 kDa) and beta (60 kDa) subunits of Ca2+/CaM kinase II in the presence or absence of exogenous substrate[2]. KN-62 in human leukemic B lymphocytes diminishes the rate of permeability increase to larger permeant cations, such as ethidium, induced by Bz-ATP, with an IC50 of 13.1 nM[4].
KN-62 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
HEK293 cells
Function assay
Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx, IC50=50.12 nM
19191585
human lymphocytes
Function assay
Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx, IC50=12.59 nM
19191585
THP1 cells
Function assay
Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA, IC50=0.081 μM
19110420
KN-62 动物研究
Animal study
KN-62 (5 mg/kg/day; ip; three times a week for 6 weeks) markedly decreases the liver metastatic tumor burden in five-week-old BALB/c athymic nude mice inoculated with TAMR-MCF-7 cells[3].KN-62 (1 μg/site, i.c.v.) blocks the antidepressant-like behavior and antidepressant-like effects of ZnCl2 (10 mg/kg, pO.)[5].
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