gne-900

GNE-900 是一种 ATP 竞争性、选择性和口服活性 ChK1抑制剂，对 ChKl,ChK2的 IC50值分别为为 0.0011，1.5 µM。GNE-900 废除 G2-M 检查点，增强 DNA 损伤，并诱导胞凋亡 (Apoptosis)。gemcitabine 和 GNE-900 给药显示抗肿瘤活性[1]< sup>。

Echothiophate is a potent, long-acting cholinesterase inhibitor used as a miotic in the treatment of glaucoma. Echothiophate covalently binds by its phosphate group to serine group at the active site of the cholinesterase. Once bound, the enzyme is permanently inactive and the cell has to make new enzymes. Echothiophate binds irreversibly to cholinesterase. Because of the very slow rate at which echothiophate is hydrolyzed by cholinesterase, its effects can last a week or more. It is used as an ocular antihypertensive in the treatment of chronic glaucoma and, in some cases, accommodative esotropia.