U73122 is an unselective PLC inhibitor. U73122 has been utilized extensively to probe PLC signalling in cells of the immune system, in neurons and in cardiomyocytes, among many other cell types. U73122 has also been used to analyse the PI(4,5)P2-dependence of ion channels during activation of the PLC pathway in native tissues and in heterologous expression systems. U73122 activates ion channels with yet unknown molecular identity in a variety of cell types. U73122 also reduces Ca2+ influx through direct actions on Ca2+ channels or indirectly by reducing the driving force for Ca2+ entry, that is, through activation of ion channels causing membrane potential depolarization. U73122 was shown to inhibit K+ channels and to induce the release of Ca2+ from intracellular stores into the cytoplasm in a PLC-independent manner[2].
作用机制
U73122 is an N-substituted maleimide, which alkylates biological nucleophils (including cysteine residues) covalently conjugating the compound to the protein. U73122 most probably inhibits PLC through such alkylation of cysteine residues.[2]
U-73122 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
human Jurkat cells
Function assay
Inhibition of human telomerase activity in human Jurkat cells by TRAP assay, IC50=0.2 μM
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