VX-984
| CAS号 | 1562396-65-9 | 货号 | BCP29319 |
| 中文名 | VX-984 | ||
| 英文名 | VX-984 | ||
| 中文别名 | |||
| 英文别名 | VX 984; VX984; M9831; M-9831; M 9831; | ||
| 分子式 | C22H19D2N7O | 分子量 | 401.46 |
| 生物活性 | VX-984, also known as M9831, is an ATP-competitive inhibitor of the catalytic subunit of DNA-dependent protein kinase (DNA-PK), with potential sensitizing and enhancing activities for both chemo- and radiotherapies. Upon administration, VX-984 binds to and inhibits the catalytic subunit of DNA-PK, thereby interfering with the non-homologous end joining (NHEJ) process and preventing repair of DNA double strand breaks (DSBs) caused by ionizing radiation or chemotherapeutic treatment. This increases chemo- and radiotherapy cytotoxicity and leads to enhanced tumor cell death. The enhanced ability of tumor cells to repair DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy; DNA-PK plays a key role in the NHEJ pathway and DSB repair. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | DNA PK | ||
结构式
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